Search Result
Results for "
oral cancer cell
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
34
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-138993A
-
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Amine N-methyltransferase
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Cancer
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NNMT-IN-6 hydrochloride (compound 78) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.6 μM. NNMT-IN-6 hydrochloride shows an inhibitory effect on the cell proliferation of the HSC-2 human oral cancer cell line .
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- HY-132846
-
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TAS0953/HM06
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RET
Apoptosis
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Cancer
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Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas .
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- HY-147402A
-
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D-0502 meglumine
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Estrogen Receptor/ERR
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Cancer
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Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
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- HY-153356
-
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Apoptosis
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Cancer
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MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
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- HY-119270
-
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Biochemical Assay Reagents
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Cancer
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PD 130908 is an orally active hypoxic cell radiosensitizer with potent radiosensitizing activity. PD 130908 can be utilized in cancer research .
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-
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- HY-116664
-
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Apoptosis
Ras
Raf
Caspase
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Cancer
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DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer .
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-
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- HY-147402
-
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D-0502
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Estrogen Receptor/ERR
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Cancer
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Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
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-
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- HY-115885
-
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HDAC
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Inflammation/Immunology
Cancer
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XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
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- HY-144318
-
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Epigenetic Reader Domain
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Cancer
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CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
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- HY-138993
-
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Amine N-methyltransferase
|
Cancer
|
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NNMT-IN-6 (compound 78) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.6 μM. NNMT-IN-6 shows an inhibitory effect on the cell proliferation of the HSC-2 human oral cancer cell line .
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- HY-164307
-
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BLU 451; LNG-451
|
EGFR
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Cancer
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Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .
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- HY-149862
-
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PROTACs
Androgen Receptor
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Cancer
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ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer .
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- HY-142772
-
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Epigenetic Reader Domain
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Cancer
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Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity .
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- HY-106789
-
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CS-684
|
Bacterial
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Infection
Inflammation/Immunology
Cancer
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Plaunotol is an orally active acyclic diterpene alcohol. Plaunotol has antibacterial activity against Helicobacter pylori which causes peptic ulcer . Plaunotol inhibits tumor angiogenesis and cell proliferation. Plaunotol induces apoptosis by activation of caspase 8 and caspase 9 pathways. Plaunotol is a potential anticancer agent against colon cancer .
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- HY-W005629
-
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Cannabinoid Receptor
PDK-1
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Metabolic Disease
Cancer
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Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells .
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- HY-16999
-
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
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- HY-19642
-
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MGCD265
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-19642A
-
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MGCD265 hydrochloride
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TAM Receptor
c-Met/HGFR
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Cancer
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Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) .
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- HY-151367
-
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ERK
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Cancer
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SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer .
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- HY-161369
-
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PROTACs
Histone Acetyltransferase
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Cancer
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CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
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- HY-146516
-
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MDM-2/p53
Apoptosis
Reactive Oxygen Species
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Cancer
|
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Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
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- HY-139990
-
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c-Fms
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Cancer
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CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity .
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- HY-10261A
-
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BIBW 2992MA2
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
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Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261
-
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BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
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Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261D
-
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BIBW 2992 oxalate
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
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Cancer
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Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261R
-
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
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Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-10261AR
-
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EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
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Cancer
|
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Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
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- HY-112823A
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HS-10296 mesylate
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EGFR
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Cancer
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Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
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- HY-112823
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HS-10296
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EGFR
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Cancer
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Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
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- HY-112823B
-
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HS-10296 hydrochloride
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EGFR
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Cancer
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Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
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- HY-112823R
-
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EGFR
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Cancer
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Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
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- HY-170403
-
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Histone Demethylase
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Cancer
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LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
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- HY-160699
-
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ULK
Ras
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Cancer
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DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can promote autophagy in lung cancer cells by inhibiting KRAS G12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects .
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- HY-118263
-
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PF-00299804 hydrate; PF-299804 hydrate
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EGFR
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Cancer
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Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC) .
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- HY-143491
-
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VEGFR
Apoptosis
Reactive Oxygen Species
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Cancer
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VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells) .
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- HY-103696
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PTC-028
1 Publications Verification
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BMI1
Apoptosis
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Cancer
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PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis .
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- HY-50895B
-
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ZD 1839 dihydrochloride
|
EGFR
Autophagy
Apoptosis
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Cancer
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Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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- HY-50895
-
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ZD1839
|
EGFR
Autophagy
Apoptosis
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Cancer
|
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Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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-
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- HY-147298
-
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CYC140
|
Polo-like Kinase (PLK)
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Cancer
|
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Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
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-
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- HY-N6642
-
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PPAR
Apoptosis
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Inflammation/Immunology
Cancer
|
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Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
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-
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- HY-156002
-
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Paluratide
|
Ras
ERK
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Cancer
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LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
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-
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- HY-119272
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EF24
1 Publications Verification
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ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species
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Inflammation/Immunology
Cancer
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EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
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-
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- HY-119198
-
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Apoptosis
Histone Methyltransferase
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Cancer
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NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
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-
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- HY-17602
-
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BBI503
|
Apoptosis
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Cancer
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Amcasertib (BBI503) is an orally activate cancer stemness kinase inhibitor that enhances apoptosis. Amcasertib inhibits the expression of NANOG and CD133 and cell viability in PC-9/GR cells.
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-
-
- HY-171450
-
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Trk Receptor
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Cancer
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TrkA-IN-9 (VMD-928) is an orally active and selective tropomyosin receptor kinase A (TrkA) inhibitor. TrkA-IN-9 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. TrkA-IN-9 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma, etc. .
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-
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- HY-162808
-
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DNA/RNA Synthesis
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Cancer
|
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GTSE1-IN-1 (compound Y18) is an orally active GTSE1 inhibitor with anticancer activity. GTSE1-IN-1 significantly inhibits cancer cell proliferation by inhibiting the transcription and expression of GTSE1, causing DNA damage and persistently inducing cell cycle arrest and cell senescence. In addition, GTSE1-IN-1 significantly inhibits the adhesion, migration and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro .
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-
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- HY-157912
-
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EGFR
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Cancer
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EGFR-IN-102 (compound 6) is an oral active EGFR inhibitor with the IC50 of 2 nM, and can be used for study of non-small-cell lung cancer .
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-
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- HY-145844
-
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EGFR
Apoptosis
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Cancer
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EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers .
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-
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- HY-N11644
-
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Others
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Cancer
|
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Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid, also known as ganoderic acid 24. Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid shows high cytotoxicity against cancer cells, such as human lung cancer cells CH27, melanoma cells M21, and oral cancer cells HSC-3 .
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-
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- HY-165245
-
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Transmembrane Glycoprotein
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Cancer
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SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
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- HY-147259
-
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c-Met/HGFR
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Cancer
|
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Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
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- HY-125677
-
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Caspase
Reactive Oxygen Species
Apoptosis
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Cancer
|
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SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
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-
- HY-108474
-
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AG 337
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Thymidylate Synthase
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Cancer
|
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Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.
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-
- HY-123024
-
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BL-S-640; SK&F 60771
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Apoptosis
Bacterial
Antibiotic
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Infection
Cancer
|
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Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
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-
- HY-50895R
-
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ZD1839 (Standard)
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EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
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-
- HY-16172
-
DMAPT
1 Publications Verification
Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
|
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect .
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-
- HY-N2486
-
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
|
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Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects.
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-
- HY-10454
-
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CEP-18770
|
Proteasome
NF-κB
Apoptosis
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Cancer
|
|
Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities .
|
-
- HY-16172A
-
|
(S)-Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
|
(S)-DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect .
|
-
- HY-N0410
-
|
Eleutheroside A; β-Sitosterol β-D-glucoside
|
Apoptosis
Reactive Oxygen Species
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-B0580B
-
|
(+)-Ketorolac
|
Ras
|
Cancer
|
|
(R)-Ketorolac is an orally active Cdc42 and Rac1 inhibitor. (R)-Ketorolac inhibits GTPase. (R)-Ketorolac alters ovarian cancer cell behaviors critical for invasion and metastasis. (R)-Ketorolac ameliorates cancer-associated cachexia .
|
-
- HY-120429
-
|
|
Apoptosis
|
Cancer
|
|
SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis .
|
-
- HY-134832
-
-
- HY-142283BS
-
|
|
EGFR
|
Cancer
|
|
N-Desmethyl dosimertinib-d5 is the deuterium labeled Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
|
-
- HY-142283CS
-
|
|
EGFR
|
Cancer
|
|
N-Methyl-dosimertinib-d5 is the deuterium labeled of Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
|
-
- HY-105634A
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-N0203
-
|
ICodonolactone; 8β-Hydroxyasterolide
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide III (ICodonolactone) is the main component of Atractylodes rhizome and has the activity of inducing apoptosis in lung cancer cells. Atractylenolide III is an orally active gastroprotective agent .
|
-
- HY-N0565
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity .
|
-
- HY-151381
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-10 is a selective, potent and orally active hDHODH inhibitor, with an IC50 value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation of cancer cells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectal cancer .
|
-
- HY-50767C
-
|
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767B
-
|
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767
-
|
PD 0332991
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-120599
-
|
VERU-111; ABI-231
|
Microtubule/Tubulin
Apoptosis
HPV
|
Cancer
|
|
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
|
-
- HY-12743A
-
|
|
Proteasome
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer .
|
-
- HY-12743
-
|
|
Proteasome
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer .
|
-
- HY-10498
-
|
CYT-997
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo . Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells .
|
-
- HY-10498A
-
|
CYT-997 dihydrochloride
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo . Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells .
|
-
- HY-163939
-
|
|
Ras
|
Cancer
|
|
RGT-018 is a potent and orally active SOS1 inhibitor with anti-tumor effects. RGT-018 exerts anti-cancer cell proliferation activity by inhibiting KRAS activation .
|
-
- HY-117996
-
|
|
CRM1
Apoptosis
|
Cancer
|
|
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity .
|
-
- HY-N1486
-
|
3-Ketoursolic acid
|
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Ursolic acid is a naturally occurring triterpenoid that has orally active. Ursolic acid induces the apoptosis of human cancer cells through multiple signaling pathways. Ursolic acid has anti-inflammatory and anticarcinogenic activity .
|
-
- HY-B0312
-
-
- HY-32345
-
|
BXL-628; Ro-26-9228
|
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells .
|
-
- HY-U00002
-
|
|
VEGFR
EGFR
|
Cancer
|
|
ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-50767D
-
|
PD 0332991 orotate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767A
-
|
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-A0065
-
|
PD 0332991 isethionate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-100888
-
|
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-149259
-
|
|
FAK
|
Cancer
|
|
FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis .
|
-
- HY-122844A
-
|
BI-853520 hydrochloride; IN-10018 hydrochloride
|
FAK
|
Cancer
|
|
Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells .
|
-
- HY-13627
-
|
|
Microtubule/Tubulin
Apoptosis
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
|
-
- HY-149408
-
|
|
Monoamine Oxidase
|
Cancer
|
|
MAOA-IN-1 (compound 15) is an orally active MAOA inhibitor with cytotoxicity against prostate cancer cells. MAOA-IN-1 has Caco-2 permeability and lower CNS permeability. MAOA-IN-1 can be further used in the research of anti-cancer and anti-inflammatory indications .
|
-
- HY-13627A
-
|
|
Apoptosis
Microtubule/Tubulin
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Estramustine phosphate, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
|
-
- HY-155785
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species
JAK
|
Cancer
|
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
|
-
- HY-14372
-
|
|
CDK
|
Cancer
|
|
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .
|
-
- HY-108713A
-
|
SHR1020 malate
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer .
|
-
- HY-129163
-
HJ-PI01
1 Publications Verification
10-Acetylphenoxazine
|
Pim
|
Cancer
|
|
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
|
-
- HY-B0223
-
-
- HY-156881
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
PARG-IN-4 (Formula (A)) is an orally active and cell-permeable PARG inhibitor. PARG-IN-4 effectively inhibits tumor growth in mouse models. PARG-IN-4 can be used in cancer research .
|
-
- HY-155163
-
-
- HY-169581
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
DIM-C-pPhtBu is an orally active endoplasmic reticulum stress activator. DIM-C-pPhtBu induces mitochondrial and lysosome dysfunction, excessive mitosis, ROS production, and unfolded protein response-mediated cell death in neck cancer cells. DIM-C-pPhtBu has antitumor activity .
|
-
- HY-15519
-
|
|
IAP
FLT3
|
Cancer
|
|
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells .
|
-
- HY-N0015
-
|
Astragaline; 3-Glucosylkaempferol; Kaempferol 3-β-D-glucopyranoside
|
Apoptosis
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Astragalin (Astragaline) a flavonoid with anti-inflammatory, antioxidant, anticancer, bacteriostatic activity. Astragalin inhibits cancer cells proliferation and migration, induces apoptosis. Astragalin is orally active and provides nerve and heart protection, and resistance against and osteoporosis .
|
-
- HY-143323
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers .
|
-
- HY-N0410R
-
|
|
Apoptosis
Reactive Oxygen Species
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-10373
-
|
CI-898
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
- HY-N0451
-
|
5,7-Dihydroxy-4'-methoxyflavone
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
|
-
- HY-10373A
-
|
CI-898 trihydrochloride
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
- HY-34544R
-
|
|
Others
|
Others
|
|
Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
- HY-W654305
-
|
PD 0332991-d4
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-N3665
-
|
|
Tyrosinase
|
Cancer
|
|
Cyclocommunol is a prenylflavonoid with antityrosinase and antiplatelet activitie, can be solated from breadfruit. Cyclocommunol exerts anti-tumor activity and inhibits the growth of human hepatoma and gastric cancer cells with IC50 values between 16 and 80 µM. Cyclocommunol shows proapoptotic effect on oral squamous cell carcinoma (OSCC) .
|
-
- HY-100507
-
-
- HY-147772
-
-
- HY-108999A
-
|
BWA770U
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999
-
|
BWA770U mesylate
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-149968
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis .
|
-
- HY-146884
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines .
|
-
- HY-B0444
-
|
|
Autophagy
Apoptosis
ERK
|
Neurological Disease
Cancer
|
|
Maprotiline hydrochloride is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects with oral activity. Maprotiline hydrochloride induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1 .
|
-
- HY-109061
-
|
YH25448; GNS-1480
|
EGFR
|
Cancer
|
|
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer .
|
-
- HY-148953
-
|
|
G-quadruplex
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
MTR-106 is a potent and orally active G-quadruplex stabilizer and RNA polymerase I inhibitor. MTR-106 induces apoptosis and inhibits cell growth. MTR-106 can be used in research of cancer .
|
-
- HY-120548
-
|
|
HSP
|
Cancer
|
|
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life .
|
-
- HY-105634AR
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate (Standard) is the analytical standard of Nomegestrol acetate. This product is intended for research and analytical applications. Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-B0965
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-145572
-
|
LY-3484356
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-109169B
-
|
IMG-7289 hydrochloride
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-145572A
-
|
LY-3484356 tosylate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-109169C
-
|
IMG-7289 dihydrochloride
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-156819
-
|
RMC-9805; KRAS G12D inhibitor 18
|
Ras
Apoptosis
|
Cancer
|
|
RMC-9805 (KRAS G12D inhibitor 18) is a potent and orally active KRAS G12D inhibitor. RMC-9805 induces apoptosis in KRAS G12D mutant cancer cells. RMC-9805 has the potential for the research of KRAS G12D mutant cancer .
|
-
- HY-10293
-
|
INCB007839; INCB7839
|
MMP
|
Cancer
|
|
Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al .
|
-
- HY-109169
-
|
IMG-7289
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-B0497
-
|
BAY2353
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
|
Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-B0497A
-
|
BAY2353 sodium
|
Antibiotic
STAT
Parasite
|
Infection
Cancer
|
|
Niclosamide (BAY2353) sodium is an orally active antihelminthic agent used in parasitic infection research . Niclosamide sodium is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide sodium has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-B0497B
-
|
BAY2353 monohydrate
|
STAT
Antibiotic
Parasite
|
Infection
Cancer
|
|
Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research . Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-163938
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
|
-
- HY-N7640
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound .
|
-
- HY-W005130
-
|
|
NF-κB
|
Metabolic Disease
Cancer
|
|
2,4,6-Trihydroxybenzaldehyde is an orally active NF- B inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity .
|
-
- HY-N2486R
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
Desoxyrhaponticin (Standard) is the analytical standard of Desoxyrhaponticin. This product is intended for research and analytical applications. Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects .
|
-
- HY-N12960
-
|
|
Apoptosis
Bcl-2 Family
Caspase
COX
MMP
STAT
|
Cancer
|
|
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
|
-
- HY-N0256
-
|
|
COX
NF-κB
|
Cancer
|
|
Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-10373B
-
|
CI-898 isethionate
|
Dihydrofolate reductase (DHFR)
Antibiotic
Antifolate
Parasite
Bacterial
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
|
-
- HY-50767R
-
|
|
CDK
|
Cancer
|
|
Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-108716
-
|
CBS9106; SL-801
|
CRM1
Apoptosis
|
Cancer
|
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .
|
-
- HY-160142
-
|
|
Btk
|
Cancer
|
|
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
|
-
- HY-17363
-
-
- HY-172251
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR-IN-17 (Compound 12l) is an orally active irreversible inhibitor of FGFR, which has a strong inhibitory effect on FGFR and its mutants. FGFR-IN-17 can inhibit the proliferation and migration, and induce apoptosis of non-small cell lung cancer cells. FGFR-IN-17 has anti-tumor activity .
|
-
- HY-160701
-
|
BLU-222
|
CDK
Apoptosis
|
Cancer
|
|
Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells .
|
-
- HY-164464
-
|
|
EGFR
|
Cancer
|
|
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .
|
-
- HY-16706
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-112870
-
|
Alflutinib; Furmonertinib; AST2818
|
EGFR
|
Cancer
|
|
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
- HY-112870A
-
|
Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
|
EGFR
|
Cancer
|
|
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
|
-
- HY-109169A
-
|
IMG-7289 ditosylate
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis .
|
-
- HY-B0497BS
-
|
BAY2353-13C6 monohydrate
|
STAT
Parasite
Antibiotic
|
Cancer
|
|
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate[1]. Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research[2]. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells[5]. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells[3][4][6].
|
-
- HY-N2510
-
|
Myristicine
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
|
-
- HY-17473
-
Embelin
4 Publications Verification
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
- HY-151623
-
ACBI2
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer .
|
-
- HY-N0565A
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hydrochloride can be used to construct gene expression regulation models .
|
-
- HY-N7083
-
Citral
1 Publications Verification
|
Parasite
|
Inflammation/Immunology
Cancer
|
|
Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects [2][3].
|
-
- HY-N0565AS
-
|
|
Isotope-Labeled Compounds
Bacterial
Antibiotic
MMP
Parasite
|
Infection
Cancer
|
|
Doxycycline-d3 hydrochloride is deuterium labeled Doxycycline (hydrochloride). Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity .
|
-
- HY-155695
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-61 (compound 12k) is a potent and orally active HDAC inhibitor. HDAC-IN-61 has anticancer active with an IC50 value of 30 nM for Bel-7402 cell. HDAC-IN-61 can be used in research of cancer .
|
-
- HY-78131C
-
|
(±)-Ibuprofen sodium
|
COX
Apoptosis
Parasite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-147308
-
|
PCLX-001
|
N-myristoyltransferase
|
Cancer
|
|
Zelenirstat is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. Zelenirstat can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma .
|
-
- HY-18614
-
|
|
Notch
γ-secretase
|
Cancer
|
|
LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC50=0.005-20 nM). LY900009 can be used for advanced cancer research .
|
-
- HY-112666
-
|
FTS amide; Salirasib amide
|
Ras
|
Cancer
|
|
Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer .
|
-
- HY-B0497C
-
|
BAY2353 olamine
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
|
Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research . Niclosamide olamin is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide olamin has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-158762
-
|
|
SHP2
|
Cancer
|
|
TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC50=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .
|
-
- HY-14653
-
|
TAC-101; Am 555S
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer .
|
-
- HY-16079
-
AZD3514
3 Publications Verification
|
Androgen Receptor
|
Cancer
|
|
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
|
-
- HY-N7271
-
|
|
RAD51
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice .
|
-
- HY-N1261
-
|
|
Others
|
Cancer
|
|
Scutebarbatine B shows significant cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, with IC50 values in the range 3.5-8.1 mM [1]<
|
-
- HY-17423E
-
|
|
HIV
Apoptosis
Reverse Transcriptase
Telomerase
|
Infection
Cancer
|
|
Abacavir hydrochloride is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir hydrochloride can inhibits the replication of HIV. Abacavir hydrochloride shows anticancer activity in prostate cancer cell lines. Abacavir hydrochloride can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-N2959
-
|
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-17423
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-N11536
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
|
-
- HY-14716
-
|
|
DNA/RNA Synthesis
Raf
|
Cancer
|
|
CCT239065 is an orally available, effective inhibitor of the mutant protein kinase V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation .
|
-
- HY-W011641
-
|
|
Potassium Channel
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Caspase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
(±)-Naringenin is an orally available anti-inflammatory agent that can regulate both acute and chronic inflammation responses, while also showing antioxidant, neuroprotective, liver-protective, and anti-cancer effects. (±)-Naringenin promotes vasodilation in endothelial cells by activating BKCa channels in muscle cells. It also exerts protective effects against experimental colitis by inhibiting Toll-like receptor 4/NF-κB signaling, making it useful in studies related to sepsis, fulminant hepatitis, fibrosis, and cancer research .
|
-
- HY-N0451R
-
|
5,7-Dihydroxy-4'-methoxyflavone (Standard)
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (Standard) is the analytical standard of Acacetin. This product is intended for research and analytical applications. Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
|
-
- HY-10338A
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .
|
-
- HY-B0223R
-
|
|
Parasite
Microtubule/Tubulin
Autophagy
Apoptosis
Reactive Oxygen Species
VEGFR
HIF/HIF Prolyl-Hydroxylase
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Albendazole (Standard) is the analytical standard of Albendazole. This product is intended for research and analytical applications. Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells .
|
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
|
-
- HY-114358
-
|
ONO-7475
|
TAM Receptor
Trk Receptor
|
Cancer
|
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
|
-
- HY-78131
-
|
(±)-Ibuprofen
|
COX
Apoptosis
Parasite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-12300A
-
|
CFI-400945 hydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
|
-
- HY-111551
-
FT113
2 Publications Verification
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Fatty Acid Synthase (FASN)
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Cancer
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FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .
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- HY-100507A
-
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CC 122 hydrochloride
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E1/E2/E3 Enzyme
Apoptosis
Molecular Glues
NF-κB
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Inflammation/Immunology
Cancer
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Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .
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- HY-N2342
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PCC1
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Apoptosis
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Cancer
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Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
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- HY-N0565B
-
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Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
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Antibiotic
MMP
Bacterial
Parasite
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Infection
Cancer
|
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Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor. Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hyclate can be used to construct gene expression regulation models .
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- HY-19822
-
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RAD1901
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Estrogen Receptor/ERR
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Cancer
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Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
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- HY-151904
-
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TAM Receptor
FLT3
PDGFR
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Cancer
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AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion .
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- HY-100399
-
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PD-132301; ATR-101
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Acyltransferase
Apoptosis
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Cancer
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Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer .
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- HY-19822A
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RAD1901 dihydrochloride
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Estrogen Receptor/ERR
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Cancer
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Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
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- HY-N0565AR
-
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MMP
Bacterial
Antibiotic
Parasite
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Infection
Cancer
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Doxycycline (hydrochloride) (Standard) is the analytical standard of Doxycycline (hydrochloride). This product is intended for research and analytical applications. Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity [4] .
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- HY-N0565R
-
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MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
|
Doxycycline (Standard) is the analytical standard of Doxycycline. This product is intended for research and analytical applications. Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity [4] .
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- HY-100399A
-
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PD-132301 hydrochloride; ATR101 hydrochloride
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Acyltransferase
Apoptosis
|
Cancer
|
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Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer .
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- HY-16706A
-
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Histone Acetyltransferase
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Cancer
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Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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- HY-B0360
-
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OPC12759; Proamipide
|
COX
|
Inflammation/Immunology
Cancer
|
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Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer .
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- HY-13270
-
|
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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- HY-N0203R
-
|
|
Apoptosis
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Neurological Disease
Inflammation/Immunology
Cancer
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|
Atractylenolide III (Standard) is the analytical standard of Atractylenolide III. This product is intended for research and analytical applications. Atractylenolide III (ICodonolactone) is the main component of Atractylodes rhizome and has the activity of inducing apoptosis in lung cancer cells. Atractylenolide III is an orally active gastroprotective agent .
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- HY-13847
-
|
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mTOR
|
Cancer
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GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
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-
- HY-N0565C
-
|
|
MMP
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
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Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline calcium can be used to construct gene expression regulation models .
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- HY-N6257
-
-
- HY-144395
-
|
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HDAC
Apoptosis
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Inflammation/Immunology
Cancer
|
|
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity .
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- HY-B0312R
-
|
|
Phosphodiesterase (PDE)
Apoptosis
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Cardiovascular Disease
Cancer
|
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Dipyridamole (Standard) is the analytical standard of Dipyridamole. This product is intended for research and analytical applications. Dipyridamole is an orally active phosphodiesterase (PDE) inhibitor. Dipyridamole also is an antiplatelet agent used in secondary prophylaxis against stroke. Dipyridamole can induce cancer cell-specific apoptosis .
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- HY-164411
-
|
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c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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- HY-169262
-
|
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Phospholipase
Apoptosis
|
Cancer
|
|
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
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-
- HY-146208
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
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- HY-161313
-
|
|
Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
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-
- HY-157210
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
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-
- HY-17583
-
-
- HY-164517
-
|
|
Trk Receptor
|
Cancer
|
|
ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research .
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- HY-B0965R
-
|
|
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine (hydrochloride) (Standard) is the analytical standard of Thioridazine (hydrochloride). This product is intended for research and analytical applications. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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-
- HY-125331
-
|
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
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-
- HY-122703
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
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-
- HY-147268
-
|
RAF/KIN_2787
|
Raf
p38 MAPK
|
Cancer
|
|
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
|
-
- HY-136990
-
|
|
Others
|
Cancer
|
|
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
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-
- HY-138751A
-
|
ASK120067 diTFA
|
EGFR
|
Cancer
|
|
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR T790M (IC50: 0.3 nM) with selectivity over EGFR WT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
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-
- HY-114338A
-
|
SHR-6390 hydrochloride
|
CDK
|
Cancer
|
|
Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
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-
- HY-12933
-
|
|
HSP
|
Cancer
|
|
BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation .
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-
- HY-114338
-
|
SHR-6390
|
CDK
|
Cancer
|
|
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
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-
- HY-76474A
-
|
|
Apoptosis
Syk
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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-
- HY-138215
-
|
|
ERK
|
Cancer
|
|
ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
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-
- HY-119906
-
|
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo .
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-
- HY-151424
-
|
|
Proteasome
|
Cancer
|
|
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
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- HY-N0256R
-
|
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COX
NF-κB
|
Cancer
|
|
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
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-
- HY-159966
-
|
|
Topoisomerase
HDAC
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
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-
- HY-113327R
-
|
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
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- HY-N6996
-
|
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Autophagy
PI3K
mTOR
Akt
|
Inflammation/Immunology
Cancer
|
|
Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury .
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- HY-N0565S3
-
-
- HY-N1109
-
Uvaol
1 Publications Verification
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Apoptosis
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Inflammation/Immunology
Cancer
|
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Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol is an orally active inducer of apoptosis in astroglioma cells. Uvaol also has anti-cancer activities. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice .
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-
- HY-109038
-
|
KRP-203 free base
|
LPL Receptor
|
Cancer
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|
Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research .
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-
- HY-18719
-
|
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Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
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Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM .
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- HY-151480
-
|
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STAT
Apoptosis
|
Cancer
|
|
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis .
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-
- HY-17423B
-
|
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HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
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-
- HY-101478
-
|
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mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .
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-
- HY-101478A
-
|
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mGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction .
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-
- HY-156677
-
|
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METTL3
|
Cancer
|
|
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
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-
- HY-B0497R
-
|
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
|
Niclosamide (Standard) is the analytical standard of Niclosamide. This product is intended for research and analytical applications. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
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-
- HY-110112
-
|
|
Integrin
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease .
|
-
- HY-129388A
-
|
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
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-
- HY-P3161
-
|
|
HSV
|
Infection
Inflammation/Immunology
Cancer
|
|
Lactoferrin from Bovine milk is a substance released by neutrophils. Lactoferrin from Bovine milk is an orally active multifunctional iron binding glycoprotein. Lactoferrin from Bovine milk prevents cell adhesion, growth and spreading of cell colonies. Lactoferrin from Bovine milk also has antiviral activity and inhibits microbial and viral adhesion and entry into host cells. Besides, Lactoferrin from Bovine milk has anti-inflammatory, immunomodulatory, and anti-cancer activities .
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-
- HY-76474
-
|
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Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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- HY-N2510R
-
|
|
5-HT Receptor
EGFR
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Myristicin (Standard) is the analytical standard of Myristicin. This product is intended for research and analytical applications. Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
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-
- HY-N0015R
-
|
|
Apoptosis
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Astragalin (Standard) is the analytical standard of Astragalin. This product is intended for research and analytical applications. Astragalin (Astragaline) a flavonoid with anti-inflammatory, antioxidant, anticancer, bacteriostatic activity. Astragalin inhibits cancer cells proliferation and migration, induces apoptosis. Astragalin is orally active and provides nerve and heart protection, and resistance against and osteoporosis .
|
-
- HY-160564
-
|
|
EGFR
|
Cancer
|
|
ZNL-0056 is an orally active ATP-competitive inhibitor that targets both the Cys797 and Cys775 in the ATP binding site of EGFR. ZNL-0056 selectively inhibits EGFR and its downstream signaling in H3255 cells. ZNL-0056 can be used for the research of cancer .
|
-
- HY-N0565BR
-
|
|
Antibiotic
MMP
Bacterial
Parasite
|
Infection
Cancer
|
|
Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate. This product is intended for research and analytical applications. Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity .
|
-
- HY-139970
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
|
-
- HY-120599A
-
|
VERU-111 hydrochloride; ABI-231 hydrochloride
|
Microtubule/Tubulin
Apoptosis
HPV
Endogenous Metabolite
|
Cancer
|
|
Sabizabulin hydrochloride is a potent orally bioavailable microtubule inhibitor with activity that interacts with the colchicine binding site. Sabizabulin hydrochloride demonstrated significant inhibition of melanoma tumor growth with an average IC50 of 5.2 nM in melanoma and prostate cancer cell lines. Pharmacological screening of Sabizabulin hydrochloride shows it has a low risk of potential side effects .
|
-
- HY-W403933R
-
|
|
Autophagy
|
Metabolic Disease
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-13691
-
|
Ro-31-7453
|
Akt
mTOR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family .
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-A0077
-
-
- HY-117136
-
|
|
HDAC
Caspase
Bcl-2 Family
|
Cancer
|
|
AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
|
-
- HY-A0077A
-
-
- HY-163938A
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: E3 ligase ligand (HY-W763812)) .
|
-
- HY-129388B
-
|
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-108232
-
|
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities .
|
-
- HY-135317
-
|
CA-4948
|
IRAK
Apoptosis
FLT3
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model
|
-
- HY-17363R
-
|
|
Keap1-Nrf2
Reactive Oxygen Species
HIV
Autophagy
Endogenous Metabolite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .
|
-
- HY-161957
-
|
|
Topoisomerase
|
Cancer
|
|
Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models .
|
-
- HY-B0568
-
|
|
Ferroptosis
HCV
Apoptosis
COX
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
|
-
- HY-17473R
-
|
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
- HY-N2420
-
-
- HY-122627
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells .
|
-
- HY-N4115
-
|
Su 3118
|
Monocarboxylate Transporter
|
Cardiovascular Disease
Cancer
|
|
Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine .
|
-
- HY-10521
-
|
SB-480848
|
Phospholipase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer .
|
-
- HY-151625
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
|
-
- HY-B0139
-
|
5-Fluorocytosine; NSC 103805; Ro 2-9915
|
Fungal
Antibiotic
|
Infection
Cancer
|
|
Flucytosine (5-Fluorocytosine) is an antifungal compound with oral activity. Flucytosine is a widely used cytotoxic drug that, after further metabolism, produces fluorinated ribonucleotides and deoxyribonucleotides, inhibits DNA and protein synthesis, and has multiple effects such as inhibiting candida and candida neoplasm infection and producies cytotoxicity to cancer cells .
|
-
- HY-162318
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
|
-
- HY-19808
-
-
- HY-138751
-
|
ASK120067
|
EGFR
|
Cancer
|
|
limertinib (ASK120067) is a potent and orally active inhibitor of EGFR T790M (IC50:0.3 nM) with selectivity over EGFR WT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-B0380A
-
|
|
Oct3/4
ERK
Akt
Apoptosis
|
Metabolic Disease
Cancer
|
|
Trimebutine maleate is an orally anti-tumor agent. Trimebutine maleate selectively suppresses stemness and proliferation of ovarian cancer stem cells (CSCs). Trimebutine maleate reduces the colonic muscle hypercontractility, modulates gastrointestinal motility, induces apoptosis and can be used for the research of glioma/glioblastoma and irritable bowel syndrome .
|
-
- HY-Y0966
-
|
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-N6884
-
Bixin
1 Publications Verification
|
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Bixin, isolated from the seeds of Bixa orellana, is an orally active carotenoid. Bixin induces apoptosis in cancer cells. Bixin possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation .
|
-
- HY-107338
-
|
Vratizolin; Wratizolin
|
HSV
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
|
|
Denotivir (Vratizolin) is an orally active antiviral agent for herpes simplex virus (HSV) and varicella-zoster virus (VZV). Denotivir inhibits the proliferation of various cancer cells, and exhibits anti-leukemic activity. Denotivir inhibits the generation of TNF-α, IL-1 and IL-6, exhibits immunosuppressive efficacy .
|
-
- HY-14543
-
-
- HY-12580
-
|
|
MDM-2/p53
|
Cancer
|
|
RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-17423A
-
|
Abacavir Hemisulfate; ABC sulfate
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-13270A
-
|
E7010 hydrochloride
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-122844
-
|
BI-853520; IN-10018
|
FAK
|
Cancer
|
|
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
|
-
- HY-12041
-
SP600125
Maximum Cited Publications
497 Publications Verification
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis .
|
-
- HY-B1334
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina .
|
-
- HY-19822S2
-
|
RAD1901-d10
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Cancer
|
|
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-B1334A
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina .
|
-
- HY-115282A
-
|
TRC-253
|
Androgen Receptor
|
Cancer
|
|
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
- HY-155787
-
|
|
CDK
|
Cancer
|
|
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
|
-
- HY-14389
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
|
-
- HY-B0520A
-
|
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Neurological Disease
Cancer
|
|
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-167114
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo .
|
-
- HY-162001
-
INX-315
1 Publications Verification
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-114657A
-
|
|
Arp2/3 Complex
|
Inflammation/Immunology
Cancer
|
|
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis .
|
-
- HY-N2959R
-
|
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-162318A
-
|
|
Molecular Glues
c-Myc
|
Cancer
|
|
MYC degrader 1 TFA (compound A80.2HCl) is an orally available MYC molecular glues degrader with anti-tumor activity. MYC degrader 1 TFA restores pRB1 protein activity and re-establishes sensitivity of MYC overexpressing cancer cells to CDK4/6 inhibitors .
|
-
- HY-145584
-
|
JPI-547/OCN-201
|
PARP
Apoptosis
Wnt
β-catenin
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Nesuparib (JPI-547) is an orally active PARP 1/2 and Tankyrase 1/2 inhibitor involved in the Wnt/β-catenin pathway. Nesuparib can induce cell cycle arrest and apoptosis and has anti-tumor activity. Nesuparib can be used to study cancer, neurological diseases and cardiovascular diseases .
|
-
- HY-A0061
-
|
Trifluorothymidine; 5-Trifluorothymidine; TFT
|
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
|
Cancer
|
|
Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
|
-
- HY-120574
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
|
-
- HY-112780
-
UC2288
5 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
|
-
- HY-B0412
-
Estriol
4 Publications Verification
Oestriol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
|
-
- HY-16397
-
|
Phenethylbiguanide
|
Mitochondrial Metabolism
AMPK
Apoptosis
|
Metabolic Disease
Cancer
|
|
Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis .
|
-
- HY-157887
-
|
|
Ras
|
Cancer
|
|
ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
|
-
- HY-126932
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
|
-
- HY-144680
-
|
ZL-2313
|
EGFR
|
Cancer
|
|
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
|
-
- HY-107592
-
|
|
IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
|
-
- HY-N7271R
-
|
|
Others
|
Cancer
|
|
Solanidine (Standard) is the analytical standard of Solanidine. This product is intended for research and analytical applications. Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice .
|
-
- HY-B2163
-
|
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
|
-
- HY-173165
-
|
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
|
Phosphatase
Apoptosis
|
Cancer
|
|
OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo .
|
-
- HY-138642
-
|
ARV-471
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-W703549
-
|
INCB007839-d3; INCB7839-d3
|
Isotope-Labeled Compounds
MMP
|
Cancer
|
|
Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
|
-
- HY-17363S1
-
|
|
Autophagy
HIV
Keap1-Nrf2
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
|
|
Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate[1]. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research[2][3].
|
-
- HY-B0497S2
-
|
BAY2353-d3
|
Isotope-Labeled Compounds
Antibiotic
STAT
Parasite
|
Infection
Cancer
|
|
Niclosamide-d3 (BAY2353-d3) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-114778
-
|
SHR3162; Fuzuloparib
|
PARP
|
Cancer
|
|
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
|
-
- HY-B0497G
-
|
BAY2353
|
Antibiotic
Parasite
STAT
|
Cancer
|
|
Niclosamide (GMP) is Niclosamide (HY-B0497) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-16594
-
|
|
Proteasome
Apoptosis
ROS Kinase
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
|
-
- HY-W012241R
-
|
|
Endogenous Metabolite
|
Others
|
|
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-124068
-
|
|
Apoptosis
GSK-3
MMP
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
Cancer
|
LQB-118 is an orally active compound derived from sandalwood. LQB-118 can inhibit the migration of glioblastoma cells and induce cell death. LQB-118 can suppress the migration and invasion of prostate cancer cells by regulating the AKT/GSK3β pathway and the expression of the MMP-9/reck genes. LQB-118 can also inhibit yeast polysaccharide-induced inflammation both in vivo and in vitro. Additionally, LQB-118 selectively induces ROS-triggered and mitochondrial-dependent apoptosis in Leishmania amazonensis. LQB-118 can be used in studies related to inflammation, infections, and cancer diseases .
|
-
- HY-129388
-
|
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-161470
-
|
|
Histone Demethylase
E1/E2/E3 Enzyme
DNA/RNA Synthesis
Caspase
Apoptosis
|
Cancer
|
|
WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-10585
-
-
- HY-78131R
-
|
|
COX
Apoptosis
Parasite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ibuprofen (Standard) is the analytical standard of Ibuprofen. This product is intended for research and analytical applications. Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-78131S2
-
|
|
Isotope-Labeled Compounds
COX
Apoptosis
Parasite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ibuprofen-d4 is a deuterium labeled Ibuprofen (HY-78131). Ibuprofen is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-145652
-
|
AMP-945
|
|
|
|
Narmafotinib (AMP-945) is an orally active inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells). Narmafotinib can be used for anti-cancer study .
|
-
- HY-17423R
-
|
|
HIV
Reverse Transcriptase
Telomerase
Apoptosis
|
Infection
Cancer
|
|
Abacavir (Standard) is the analytical standard of Abacavir. This product is intended for research and analytical applications. Abacavir is an orally active and competitive nucleoside reverse transcriptase inhibitor. Abacavir can inhibits the replication of HIV. Abacavir shows anticancer activity in prostate cancer cell lines. Abacavir can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-B0520
-
|
Benzatropine; Benzotropine
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
|
|
Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-156784
-
|
DHX9-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
|
ATX968 (example 31) is an orally active, potent and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with the EC50 of 0.054 μM in circBRIP1. ATX968 results in robust and durable tumor growth inhibition or regression in mouse xenograft studies with MSI-H/dMMR colorectal cancer cell lines .
|
-
- HY-147261
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines .
|
-
- HY-13591
-
|
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
|
-
- HY-109523
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- HY-12768B
-
|
BLZ945 dihydrochloride
|
c-Fms
|
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
|
-
- HY-116248
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
|
-
- HY-N7083R
-
|
|
Apoptosis
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
Cancer
|
|
Citral (Standard) is the analytical standard of Citral. This product is intended for research and analytical applications. Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects .
|
-
- HY-12908
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL) .
|
-
- HY-151504
-
|
ALM301
|
Akt
|
Cancer
|
|
Engasertib is an orally active highly specific AKT inhibitor with IC50 values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. Engasertib inhibits AKT phosphorylation and modulates downstream signalling in vitro. Engasertib can inhibit cancer cell proliferation and tumor growth .
|
-
- HY-108713
-
|
SHR1020
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-N6257R
-
-
- HY-10261E
-
|
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-138642A
-
|
(Rac)-ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-163616
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-N7140
-
|
γ-Linolenic acid
|
Endogenous Metabolite
Apoptosis
NF-κB
ERK
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases .
|
-
- HY-A0077S2
-
-
- HY-144088
-
|
HPK1-IN-22
|
MAP4K
|
Inflammation/Immunology
Cancer
|
|
ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a +CD8 + T cells, but not T cells, PD-1 +CD8 + T cells, TIM-3 +CD8 + Infiltration of T cells and LAG3 +CD8 + T cells was reduced .
|
-
- HY-164476
-
|
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-100586
-
|
(±) -Ibuprofen L-lysine
|
COX
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Ibuprofen ((±)-Ibuprofen) L-lysine is a potent orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen L-lysine inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen L-lysine is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen L-lysine can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-170792
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-48 (compound D3) is an orally effective PRMT5 inhibitor (IC50=20.7 nM) with anticancer activity. PRMT5-IN-48 can inhibit the growth of various cancer cells, induce apoptosis (apoptosis), and arrest the cell cycle at the G0/G1 phase. PRMT5-IN-48 can be used for non-Hodgkin lymphoma (NHL) research .
|
-
- HY-78131CS
-
|
(±)-Ibuprofen-d3 sodium
|
Apoptosis
COX
Isotope-Labeled Compounds
Parasite
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ibuprofen-d3 ((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-168968S
-
|
|
EGFR
Histone Demethylase
|
Cancer
|
|
ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
|
-
- HY-151595
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome) .
|
-
- HY-142076A
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
|
-
- HY-10585AG
-
|
Sodium Valproate (sodium)
|
Organoid
HDAC
Autophagy
Mitophagy
HIV
Notch
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-142076
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
|
-
- HY-N2342R
-
|
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 (Standard) is the analytical standard of Procyanidin C1. This product is intended for research and analytical applications. Procyanidin C1 (PCC1), a natural polyphenol with oral activity, causes DNA damage, cell cycle arrest and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells. Procyanidin C1 shows senotherapeutic activity and increases lifespan in mice .
|
-
- HY-10585A
-
|
Sodium Valproate sodium
|
Organoid
HDAC
Autophagy
Mitophagy
HIV
Notch
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-162133
-
|
|
STING
|
Cancer
|
|
MSA-2-Pt is an orally active STING agonist that has good cell membrane permeability. MSA-2-Pt can induce cell death by Pt, which may release damaged DNA to activate the cGAS-STING pathway. Besides, MSA-2-Pt can activate the STING pathway directly by MSA-2. MSA-2-Pt can be used for the research of cancer .
|
-
- HY-10357
-
|
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities .
|
-
- HY-111784
-
|
CCS1477
|
Epigenetic Reader Domain
|
Cancer
|
|
Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
|
-
- HY-170934
-
|
|
FGFR
|
Cancer
|
|
BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable
pharmacokinetic properties with an oral bioavailability of 29 % in mice .
|
-
- HY-146565
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
|
-
- HY-115282
-
|
TRC-253 free base
|
Androgen Receptor
|
Cancer
|
|
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
- HY-157838
-
|
|
MAP4K
|
Cancer
|
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
|
-
- HY-149843
-
|
|
FGFR
PROTACs
|
Cancer
|
|
LC-MB12 is an orally active PROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
|
-
- HY-119217
-
AZ084
2 Publications Verification
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma . AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer .
|
-
- HY-170905S
-
-
- HY-151968
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
|
-
- HY-147040
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC50 of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC50 of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity .
|
-
- HY-142283AS
-
|
|
EGFR
|
Cancer
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-112198
-
|
|
ATM/ATR
|
Cancer
|
|
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer .
|
-
- HY-10885
-
|
ABT-472
|
PARP
|
Cancer
|
|
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
|
-
- HY-124403
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-129458
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- HY-B1037
-
|
Albuterol; AH-3365
|
Adrenergic Receptor
ERK
|
Inflammation/Immunology
Cancer
|
|
Salbutamol (Albuterol) is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-145655
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
|
-
- HY-143430
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) is an orally active CDC7 kinase inhibitor. (S)-LY3177833 shows broad in vitro anticancer activity .
|
-
- HY-143430A
-
|
|
CDK
|
Cancer
|
|
(S)-LY3177833 ((S)-Example 2) hydrate is an orally active CDC7 kinase inhibitor. (S)-LY3177833 hydrate shows broad in vitro anticancer activity .
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-161644
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
|
-
- HY-173048
-
|
|
ClpP
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC50 of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC50 of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-N6954
-
|
|
ATM/ATR
STAT
CDK
Hedgehog
|
Inflammation/Immunology
Cancer
|
|
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-N6884R
-
|
|
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Bixin (Standard) is the analytical standard of Bixin. This product is intended for research and analytical applications. Bixin, isolated from the seeds of Bixa orellana, is an orally active carotenoid. Bixin induces apoptosis in cancer cells. Bixin possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation.
|
-
- HY-50901
-
|
AE 3-208
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer .
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-B1037B
-
|
Albuterol adipate; AH-3365 adipate
|
Adrenergic Receptor
ERK
|
Inflammation/Immunology
Cancer
|
|
Salbutamol (Albuterol) adipate is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol adipate promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol adipate is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-111193
-
|
3-Chloroprocainamide
|
NF-κB
Apoptosis
|
Cancer
|
|
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
|
-
- HY-50901A
-
|
AE 3-208 sodium salt
|
Prostaglandin Receptor
|
Endocrinology
Cancer
|
|
ONO-AE3-208 (sodium salt) is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 (sodium salt) shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 (sodium salt) suppresses cell invasion, migration, and metastasis of prostate cancer .
|
-
- HY-101761
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-121619
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Jacaric acid is a conjugated linolenic acid, which inhibits viability in cells PC-3 (IC50 is 11.8 μM), LNCaP (IC50 is 2.2 μM) and DLD-1, induces apoptosis and necrosis . Jacaric acid exhibits anticaner activity against prostate cancer and adenocarcinoma . Jacaric acid exhibits immunomodulating activity in murine peritoneal macrophages as an immunopotentiator . Jacaric acid is orally active.
|
-
- HY-170952
-
|
|
Molecular Glues
|
Cancer
|
|
LYG-409 is an orally active degrader of GSPT1. LYG-409 shows excellent anti-acute myeloid leukemia and prostate cancer in vivo with TGI of 94.34% and 104.49%, respectively. LYG-409 inhibits KG-1 cells mediated by the degradation of GSPT1 with an IC50 of 9.50 nM, with a DC50 of 7.87 nM in vitro .
|
-
- HY-N2181
-
|
|
Cytochrome P450
Apoptosis
Bacterial
Autophagy
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
|
-
- HY-A0077R
-
-
- HY-172392
-
|
|
MNK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro .
|
-
- HY-N3248
-
|
Momordicacoside G
|
Endogenous Metabolite
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Momordicoside G (Momordicacoside G) is an orally active cucurbitane-type triterpene glycoside. Momordicoside G selectively induces apoptosis of M1-like macrophages, without affecting M2-like macrophages. Momordicoside G reduces intracellular ROS levels and promotes autophagy. Momordicoside G also has anticancer activity, inhibiting the growth of cancer cell lines. Momordicoside G stimulates M2-associated lung injury repair and prevents inflammatory lung cancer injury .
|
-
- HY-135317F
-
|
CA-4948 phosphate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model .
|
-
- HY-B0568R
-
|
|
Ferroptosis
HCV
Apoptosis
COX
|
Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Deferiprone (Standard) is the analytical standard of Deferiprone. This product is intended for research and analytical applications. Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
|
-
- HY-10585B
-
|
VPA (sodium)(2:1); 2-Propylpentanoic Acid (sodium)(2:1)
|
HDAC
Autophagy
Mitophagy
HIV
Notch
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-135317E
-
|
CA-4948 maleate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model .
|
-
- HY-144269
-
|
|
Raf
|
Cancer
|
|
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
|
-
- HY-12033
-
|
2-ME2; NSC-659853
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-135317C
-
|
CA-4948 tosylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model .
|
-
- HY-155065
-
|
|
Reactive Oxygen Species
Apoptosis
CDK
|
Cancer
|
|
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
|
-
- HY-A0059
-
|
NF 113; SAP 113; Methylmercadone
|
Bacterial
Parasite
Antibiotic
Fungal
Apoptosis
STAT
Interleukin Related
TNF Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
Nifuratel (NF 113) is an orally active broad-spectrum antibiotic with antiprotozoal, antibacterial, anticancer and anti-inflammatory activities, and has good inhibitory effects on Candida and Trichomonas. Nifuratel is also a STAT3 inhibitor, which significantly inhibits the growth and proliferation of human gastric cancer cells and induces apoptosis. In addition, Nifuratel also inhibits mast cell-mediated antigen hypersensitivity reactions and can be used in the study of IgE-mediated allergic diseases .
|
-
- HY-135317B
-
|
CA-4948 hydrochloride
|
IRAK
FLT3
Apoptosis
NF-κB
MyD88
|
Inflammation/Immunology
Cancer
|
|
Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model .
|
-
- HY-78131S3
-
|
(±)-Ibuprofen-13C6
|
Isotope-Labeled Compounds
Apoptosis
Parasite
COX
|
Cancer
|
|
Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
|
-
- HY-17013A
-
|
MS-209
|
P-glycoprotein
|
Cancer
|
|
Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
|
-
- HY-135317D
-
|
CA-4948 mesylate
|
IRAK
FLT3
NF-κB
MyD88
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model .
|
-
- HY-170576
-
|
|
FLT3
STAT
Apoptosis
|
Cancer
|
|
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
|
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-114906
-
|
|
Sirtuin
|
Cancer
|
|
SIRT1/2/3-IN-2 (compound 9) is a potent SIRT inhibitor, with inhibition rates of 27%, 72%, and 71% targeting SIRT1, SIRT2, and SIRT3, respectively, at 200 μM. SIRT3 is a potential tumor suppressor or promoter, and its increased transcription may be associated with lymph node-positive breast cancer and oral squamous cell carcinoma .
|
-
- HY-B0380AR
-
|
|
Oct3/4
ERK
Akt
Apoptosis
|
Metabolic Disease
Cancer
|
|
Trimebutine (maleate) (Standard) is the analytical standard of Trimebutine (maleate). This product is intended for research and analytical applications. Trimebutine maleate is an orally anti-tumor agent. Trimebutine maleate selectively suppresses stemness and proliferation of ovarian cancer stem cells (CSCs). Trimebutine maleate reduces the colonic muscle hypercontractility, modulates gastrointestinal motility, induces apoptosis and can be used for the research of glioma/glioblastoma and irritable bowel syndrome .
|
-
- HY-153855
-
|
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research .
|
-
- HY-N6996R
-
|
|
Autophagy
PI3K
mTOR
Akt
|
Inflammation/Immunology
Cancer
|
|
Methyl Eugenol (Standard) is the analytical standard of Methyl Eugenol. This product is intended for research and analytical applications. Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury .
|
-
- HY-134463
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-15856B
-
|
Flupenthixol dihydrochloride
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-150654
-
|
|
WDR5
|
Cancer
|
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
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-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-B0139R
-
|
5-Fluorocytosine (Standard); NSC 103805 (Standard); Ro 2-9915 (Standard)
|
Fungal
Antibiotic
|
Infection
Cancer
|
|
Flucytosine (Standard) is the analytical standard of Flucytosine. This product is intended for research and analytical applications. Flucytosine (5-Fluorocytosine) is an antifungal compound with oral activity. Flucytosine is a widely used cytotoxic drug that, after further metabolism, produces fluorinated ribonucleotides and deoxyribonucleotides, inhibits DNA and protein synthesis, and has multiple effects such as inhibiting candida and candida neoplasm infection and producies cytotoxicity to cancer cells .
|
-
- HY-18750A
-
|
AZD3759 hydrochloride
|
EGFR
Apoptosis
|
Cancer
|
|
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .
|
-
- HY-155105
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-Y0966R
-
|
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine (Standard) is the analytical standard of Glycine. This product is intended for research and analytical applications. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-15856A
-
|
Flupenthixol
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-173117
-
|
|
CaMK
|
Cardiovascular Disease
Cancer
|
|
RA306 is an orally active CAMK2 inhibitor. RA306 can block the PEAK1/CAMK2 signaling pathway. RA306 inhibits the proliferation, migration, and invasion of breast cancer cells and has anti-tumor activity. In addition, RA306 can improve dilated cardiomyopathy in mice and can be used in the research of heart diseases .
|
-
- HY-18696
-
|
|
c-Met/HGFR
Caspase
Apoptosis
|
Cancer
|
|
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis .
|
-
- HY-B2163R
-
|
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Astaxanthin (Standard) is the analytical standard of Astaxanthin. This product is intended for research and analytical applications. Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
|
-
- HY-153066
-
|
KIF18A-IN-7
|
Kinesin
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
|
-
- HY-17013
-
|
MS-209 free base
|
P-glycoprotein
|
Cancer
|
|
Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
|
-
- HY-149005
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
|
-
- HY-13265
-
AR-42
2 Publications Verification
HDAC-42; OSU-HDAC42
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
|
-
- HY-10585R
-
|
Dipropylacetic Acid (Standard)
|
Organoid
HDAC
Autophagy
Mitophagy
HIV
Notch
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Valproic acid (Dipropylacetic Acid) (Standard) is an analytical standard for valproic acid. This product is intended for research and analytical applications. Valproic acid is an orally active HDAC inhibitor (IC50=0.5-2 mM), inhibits the activity of HDAC1 (IC50=400 μM), and induces the degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits the proliferation of small cell lung cancer (SCLC) cells. Valproic acid is used in the study of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and migraine .
|
-
- HY-17013D
-
|
MS-209 sesquifumarate
|
P-glycoprotein
|
Cancer
|
|
Dofequidar (MS-209) sesquifumarate is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar sesquifumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar sesquifumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
|
-
- HY-169403
-
|
|
STAT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
|
-
- HY-111237
-
|
Olomoucin
|
CDK
NF-κB
PERK
Bcl-2 Family
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research .
|
-
- HY-10585AR
-
|
|
Organoid
HDAC
Autophagy
Mitophagy
HIV
Notch
Apoptosis
Endogenous Metabolite
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Valproic acid (sodium) (Standard) is the analytical standard of Valproic acid (sodium). This product is intended for research and analytical applications. Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-119307
-
|
TMI-005
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17423AR
-
|
|
Reverse Transcriptase
HIV
Telomerase
Apoptosis
|
Infection
|
|
Abacavir (sulfate) (Standard) is the analytical standard of Abacavir (sulfate). This product is intended for research and analytical applications. Abacavir sulfate (Abacavir Hemisulfate) is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir sulfate can inhibits the replication of HIV. Abacavir sulfate shows anticancer activity in prostate cancer cell lines. Abacavir sulfate can trespass the blood-brain-barrier and suppresses telomerase activity .
|
-
- HY-18750
-
|
AZD3759
|
EGFR
Apoptosis
|
Cancer
|
|
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
|
-
- HY-B0364A
-
|
Dyclocaine hydrochloride
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Infection
Cancer
|
|
Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
|
-
- HY-158027
-
|
|
Raf
VEGFR
FGFR
|
Cancer
|
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer .
|
-
- HY-B0520AR
-
|
Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Neurological Disease
Cancer
|
|
Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-A0061R
-
|
|
Thymidylate Synthase
HSV
Nucleoside Antimetabolite/Analog
Orthopoxvirus
DNA/RNA Synthesis
Apoptosis
Autophagy
|
Cancer
|
|
Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors .
|
-
- HY-19939S
-
VX-984
4 Publications Verification
M9831
|
DNA-PK
|
Cancer
|
|
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-Y1117
-
|
|
Apoptosis
TGF-β Receptor
NF-κB
COX
NADPH Oxidase
ROS Kinase
|
Neurological Disease
Inflammation/Immunology
|
|
Melamine is an orally active inducer of Apoptosis. Melamine induces animal disease models. Melamine affects the activity of Sertoli cell and can be used for research on male reproductive function. Melamine also has neurotoxicity and nephrotoxicity. Melamine induces cognitive impairment and acute kidney injury models. Melamine can also be used to induce bladder cancer and urinary stone models .
|
-
- HY-19822S3
-
|
RAD1901-d6
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-10409
-
|
TG-101348; SAR 302503
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-10409A
-
|
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-111158
-
|
|
c-Met/HGFR
|
Cancer
|
|
BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
|
-
- HY-N3980R
-
|
|
Autophagy
RAD51
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-B0367
-
|
Chlortenoxicam; Ro 13-9297
|
Apoptosis
COX
NO Synthase
Interleukin Related
Prostaglandin Receptor
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer .
|
-
- HY-136895
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM) .
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
|
-
- HY-144448
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
|
-
- HY-W326094
-
|
GOE 1734; PD 104 208; NSC 328786
|
DNA/RNA Synthesis
|
Cancer
|
|
Dinaline (GOE 1734; PD 104 208; NSC 328786) is a potent and orally activity anticancer agent. Dinaline shows cytotoxicity and antitumor activity. Dinaline has the potential for the research of colorectal cancer .
|
-
- HY-114319
-
|
|
Others
|
Cancer
|
|
β-Cembrenediol is a potent and orally active anticancer agent. β-Cembrenediol shows phytotoxic activities. β-Cembrenediol reduces the migration and colony formation. β-Cembrenediol decreases the protein expression of TDO2, IDO1. β-Cembrenediol has the potential for the research of prostate cancer .
|
-
- HY-W015828
-
|
RGX-202; 3-Guanidinopropionic acid
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Ompenaclid (RGX-202) is an oral small-molecule SLC6A8 transporter inhibitor. Ompenaclid robustly inhibits creatine import in vitro and in vivo, reduces intracellular phosphocreatine and ATP levels, and induces tumor apoptosis. Ompenaclid can be used for the research of cancer and duchenne muscular dystrophy .
|
-
- HY-P2385
-
-
- HY-116452
-
|
|
VEGFR
|
Cancer
|
|
YLT192 is an orally active and highly bioavailable VEGFR2 inhibitor with potent anti-angiogenic activity and anti-tumor efficacy. YLT192 significantly inhibited the kinase activity of VEGFR2 and inhibited the proliferation, migration, invasion and tube formation of human umbilical cord vascular endothelial cells. YLT192 also inhibited VEGF-induced VEGFR2 phosphorylation and its downstream signaling regulators. YLT192 also showed the ability to inhibit angiogenesis in vivo in zebrafish embryo models and alginate-coated tumor cell experiments. YLT192 can directly inhibit the proliferation of cancer cells and induce their apoptosis .
|
-
- HY-147682
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-155491
-
|
|
Bacterial
|
Cancer
|
|
Antibacterial agent 166 (Compound 19q), a derivative of Nitisinone (HY-B0607), is a selective and orally active Fusobacterium nucleatum inhibitor with a MIC50 of 1 μg/mL. Antibacterial agent 166 effectively attenuates the migratory ability of MC-38 cells induced by Fusobacterium nucleatum. Antibacterial agent 166 is a promising anti-F. nucleatum lead compound and can be used for colorectal cancer (CRC) research .
|
-
- HY-13027
-
|
GSI-IX
|
Organoid
γ-secretase
Amyloid-β
Autophagy
Notch
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment .
|
-
- HY-160613
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
|
-
- HY-145734A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
|
-
- HY-B0520AS1
-
|
|
Dopamine Receptor
Histamine Receptor
mAChR
|
Cancer
|
|
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
|
-
- HY-145574
-
|
WX-0593
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
BCRP
Akt
ERK
STAT
|
Cancer
|
|
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer .
|
-
- HY-12794
-
|
|
PI3K
Autophagy
|
Neurological Disease
Cancer
|
|
Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC50=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs) .
|
-
- HY-145734
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-108713R
-
|
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-15160A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15160B
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-103018
-
|
ASN-002
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-103457
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
|
-
- HY-109523S
-
|
|
Ferroptosis
HMG-CoA Reductase (HMGCR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- HY-19822S
-
|
RAD1901-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-103018A
-
|
ASN-002 hydrochloride
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
|
Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-134884
-
|
PD-1/PD-L1-IN-8
|
PD-1/PD-L1
|
Cancer
|
|
INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research .
|
-
- HY-114277
-
|
AMG-510
|
Ras
|
Cancer
|
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-40161
-
|
|
Endogenous Metabolite
Bacterial
|
Metabolic Disease
Cancer
|
|
Indole-3-carboxylic acid is an orally active urinary indolic tryptophan metabolite. Indole-3-carboxylic acid is a mediator of priming against Plectosphaerella cucumerina. Indole-3-carboxylic acid enhances the anti-colorectal cancer potency of Doxorubicin (HY-15142A) by inducing cell senescence. Indole-3-carboxylic acid can be used in liver disease research .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-100574A
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-120149
-
|
|
Toll-like Receptor (TLR)
MDM-2/p53
MMP
Caspase
SOD
p38 MAPK
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50 in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active .
|
-
- HY-164525
-
|
SC-81490; PF-02881307
|
MMP
|
Cancer
|
|
SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with Ki values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research .
|
-
- HY-100574
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-146138
-
|
|
EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
|
-
- HY-N6954R
-
|
|
ATM/ATR
STAT
CDK
Hedgehog
|
Cancer
|
|
Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
|
-
- HY-163396
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-12678R
-
|
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-120356
-
|
TAI-95
|
Apoptosis
NEKs
|
Cancer
|
|
T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models .
|
-
- HY-B0520AS
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
mAChR
Histamine Receptor
|
Neurological Disease
Cancer
|
|
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
|
-
- HY-117025A
-
|
Keramamine A hydrochloride
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1 .
|
-
- HY-12972
-
|
PF-06747775
|
EGFR
|
Cancer
|
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-162702
-
|
|
Androgen Receptor
PROTACs
|
Cancer
|
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
|
-
- HY-117025
-
|
Keramamine A
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1 .
|
-
- HY-B1037R
-
|
Albuterol (Standard); AH-3365 (Standard)
|
Adrenergic Receptor
ERK
|
Inflammation/Immunology
Cancer
|
|
Salbutamol (Standard) is the analytical standard of Salbutamol. This product is intended for research and analytical applications. Salbutamol (Albuterol) is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-16749A
-
|
PLX-3397 hydrochloride
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity .
|
-
- HY-N0447
-
|
|
TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-157913
-
|
|
Pyruvate Kinase
Apoptosis
|
Cancer
|
|
PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
|
-
- HY-103387
-
|
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects .
|
-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
|
-
- HY-173084
-
|
|
Phosphatase
MDM-2/p53
|
Cancer
|
|
BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes .
|
-
- HY-116749
-
|
BBSKE
|
TrxR
|
Cancer
|
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
|
-
- HY-163719
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy .
|
-
- HY-15856BR
-
|
Flupenthixol dihydrochloride (Standard)
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
|
Flupentixol (dihydrochloride) (Standard) is the analytical standard of Flupentixol (dihydrochloride). This product is intended for research and analytical applications. Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-169054
-
|
|
TSH Receptor
|
Cancer
|
|
NCATS-SM4420 (Compound A35) is an orally active thyroid-stimulating hormone receptor (TSHR) ligand that inhibits the proliferation of MDA-T32 and MDA-T85 cells in vitro (IC50 values of 0.71 μM and 0.38 μM, respectively) and suppresses metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds promise for research in the field of thyroid cancer .
|
-
- HY-W011258
-
|
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cancer
|
|
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-N0108
-
|
Parietin; Rheochrysidin
|
Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
|
-
- HY-P5557
-
|
|
Bacterial
Necroptosis
|
Cancer
|
|
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells .
|
-
- HY-B0493
-
|
|
Chloride Channel
COX
|
Inflammation/Immunology
Cancer
|
|
Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-A0033
-
|
UK-88525
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-15614A
-
|
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .
|
-
- HY-144310
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Cancer
|
|
DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer .
|
-
- HY-170527
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
|
-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-15614
-
|
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .
|
-
- HY-N6973
-
Boldine
1 Publications Verification
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
|
-
- HY-15306S
-
|
SB-497115-13C4
|
Thrombopoietin Receptor
Bacterial
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
|
-
- HY-162356
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
|
-
- HY-14397G
-
|
Indometacin
|
Antibiotic
Influenza Virus
Bacterial
COX
|
Cancer
|
|
Indomethacin (GMP) is Indomethacin (HY-14397) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research .
|
-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-163479
-
|
|
Eukaryotic Initiation Factor (eIF)
MNK
|
Cancer
|
|
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970) .
|
-
- HY-103712B
-
|
CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-156671
-
|
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
|
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
|
-
- HY-145685
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer .
|
-
- HY-168716
-
|
|
Ras
|
Cancer
|
|
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .
|
-
- HY-12033S2
-
|
2-ME2-d5; NSC-659853-d5
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
|
-
- HY-100574B
-
|
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Inflammation/Immunology
Cancer
|
|
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model .
|
-
- HY-N0316
-
|
|
JAK
NF-κB
Reactive Oxygen Species
Apoptosis
VEGFR
c-Myc
|
Cancer
|
|
Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-B1971
-
-
- HY-116000
-
|
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-B1971R
-
-
- HY-170978
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
|
-
- HY-173059
-
|
|
CDK
|
Cancer
|
|
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
|
-
- HY-12033S
-
|
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
|
-
- HY-12033S1
-
|
2-ME2-13C6; NSC-659853-13C6
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
|
-
- HY-168650
-
|
|
ROCK
HDAC
|
Inflammation/Immunology
Cancer
|
|
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
|
-
- HY-13559
-
|
Azaspirane
|
Apoptosis
|
Cancer
|
|
Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
|
-
- HY-139612
-
|
JDQ-443; NVP-JDQ443
|
Ras
PERK
|
Cancer
|
|
Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity .
|
-
- HY-139612A
-
|
(S)-NVP-JDQ443
|
Ras
PERK
|
Cancer
|
|
(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity .
|
-
- HY-B0364AR
-
|
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Infection
Cancer
|
|
Dyclonine (hydrochloride) (Standard) is the analytical standard of Dyclonine (hydrochloride). This product is intended for research and analytical applications. Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
|
-
- HY-144437
-
|
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
|
-
- HY-A0012
-
|
UK-88525 hydrobromide
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-18187
-
|
|
Apoptosis
|
Cancer
|
|
Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
|
-
- HY-114770
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-142283
-
|
|
Isotope-Labeled Compounds
EGFR
|
Cancer
|
|
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-158031
-
|
|
Apoptosis
Polo-like Kinase (PLK)
Epigenetic Reader Domain
|
Cancer
|
|
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .
|
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-B0239
-
|
|
Antibiotic
Bacterial
HIF/HIF Prolyl-Hydroxylase
VEGFR
Autophagy
Apoptosis
Beclin1
JNK
Akt
MMP
|
Infection
Cancer
|
|
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
|
-
- HY-115630
-
|
|
RIP kinase
Caspase
Apoptosis
|
Cancer
|
|
cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models .
|
-
- HY-N3945
-
|
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-N0316R
-
|
|
JAK
NF-κB
Reactive Oxygen Species
Apoptosis
VEGFR
c-Myc
|
Cancer
|
|
Mollugin (Standard) is the analytical standard of Mollugin. This product is intended for research and analytical applications. Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway .
|
-
- HY-167854
-
|
|
Aurora Kinase
Apoptosis
IGF-1R
|
Cancer
|
|
KW-2450 Free base is a potent multikinase inhibitor targeting Aurora A and B kinases, demonstrating significant antitumor activity against triple-negative breast cancer (TNBC). KW-2450 Free base effectively reduces cell viability, promotes apoptosis, and inhibits colony formation and mammosphere formation in TNBC cells. KW-2450 Free base significantly suppresses the growth of TNBC xenografts, leading to tetraploid accumulation followed by apoptosis or the survival of octaploid cells. KW-2450 Free base enhances the efficacy of combination therapy with the MEK inhibitor selumetinib, resulting in a synergistic antitumor effect in TNBC models. KW-2450 Free base also acts as an orally bioavailable inhibitor of IGF-1R and IR tyrosine kinases, contributing to its potential antineoplastic activity by inhibiting tumor cell proliferation and inducing apoptosis.
|
-
- HY-145835A
-
|
|
PERK
|
Infection
Cancer
|
|
(S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM .
|
-
- HY-144614
-
|
|
DYRK
Apoptosis
|
Neurological Disease
Cancer
|
|
JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
|
-
- HY-168267
-
|
|
Deubiquitinase
|
Infection
Cancer
|
|
XH161-180 is a potent and orally active ubiquitin carboxyl-terminal hydrolase 2 (USP2) inhibitor. XH161-180 decreases the protein of cyclin D and ACE2. XH161-180 shows antiproliferative activity. XH161-180 has the potential for the research of cancer and virus infection depending on ACE2 .
|
-
- HY-19617A
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-19617B
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-19617
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-135699
-
TD52
1 Publications Verification
|
Apoptosis
Phosphatase
Akt
|
Cancer
|
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-135699A
-
|
|
Akt
Phosphatase
Apoptosis
|
Cancer
|
|
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N6866
-
|
|
Apoptosis
AMPK
Akt
PERK
Keap1-Nrf2
Caspase
PARP
GSK-3
NO Synthase
Interleukin Related
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease .
|
-
- HY-12279A
-
|
TGR-1202 tosylate; RP5264 tosylate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .
|
-
- HY-12279C
-
|
TGR-1202 hydrochloride; RP5264 hydrochloride
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
|
-
- HY-158113
-
|
|
Histone Acetyltransferase
PROTACs
|
Cancer
|
|
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
|
-
- HY-168491
-
|
|
Phosphodiesterase (PDE)
STING
PD-1/PD-L1
|
Cancer
|
|
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .
|
-
- HY-114277S
-
|
AMG-510-d7
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-10226
-
|
R306465
|
Apoptosis
HDAC
|
Cancer
|
|
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases
the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-120356A
-
|
TAI-95 tosylate
|
NEKs
Apoptosis
|
Cancer
|
|
T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models .
|
-
- HY-148561
-
|
|
CDK
GSK-3
PKC
|
Cancer
|
|
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent .
|
-
- HY-135805
-
|
|
EGFR
|
Cancer
|
|
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
|
-
- HY-D0848
-
|
Bisacrylamide; MBA; Methylenebisacrylamide; N,N-Methylenebisacrylamide
|
Biochemical Assay Reagents
MDM-2/p53
Caspase
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
N,N'-Methylenebisacrylamide (Bisacrylamide) is an orally active acrylamide dimer and crosslinker. N,N'-Methylenebisacrylamide increases CYP2E1, P53, cleaved caspase-3. N,N'-Methylenebisacrylamide promotes hepatic cancer. N,N'-Methylenebisacrylamide changes sperm abnormality rate and sperm count. N,N'-Methylenebisacrylamide decreases the number of various cells in the blood as well as induces liver and testicular damage. N,N'-Methylenebisacrylamide is used to prepare polyacrylamide gel .
|
-
- HY-N0234
-
|
7-O-Methylbavachin; Bavachinin A
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cancer
|
|
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-114277S2
-
|
AMG-510-d3
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
|
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
|
-
- HY-16637D
-
|
Vitamin B9 disodium; Vitamin M disodium
|
Endogenous Metabolite
DNA/RNA Synthesis
|
Others
Neurological Disease
Cancer
|
|
Folic acid disodium (Vitamin B9 disodium; Vitamin M disodium) is an orally active disodium salt form of Folic acid (HY-16637) with an intrinsic dissolution rate (IDR) of 4.96·10 5 g/s . Folic acid disodium serves as cofactor in single-carbon transfer reactions and exhibits protective effects against neural tube defects, ischemic events, and cancer. Folate acid disodium overload leads to impaired brain development in embryogenesis and promotes growth of precancerous altered cells. Folic acid deficiency leads to megaloblastic anemia .
|
-
- HY-10409S
-
|
TG-101348-d9; SAR 302503-d9
|
Isotope-Labeled Compounds
Apoptosis
JAK
|
Cancer
|
|
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-12678S
-
|
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-115904
-
|
|
CDK
FLT3
|
Cancer
|
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
- HY-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-B0239R
-
|
|
Antibiotic
Bacterial
HIF/HIF Prolyl-Hydroxylase
VEGFR
Autophagy
Apoptosis
Beclin1
JNK
Akt
MMP
|
Infection
Cancer
|
|
Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
|
-
- HY-126257
-
|
|
Akt
Apoptosis
|
Cancer
|
|
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
|
-
- HY-104048
-
|
|
Histone Demethylase
|
Cancer
|
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-164468
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
|
|
Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087) .
|
-
- HY-N0704
-
|
|
Sirtuin
PPAR
Fatty Acid Synthase (FASN)
c-Myc
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27 .
|
-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
|
-
- HY-B0493R
-
|
|
Chloride Channel
COX
|
Inflammation/Immunology
|
|
Niflumic acid (Standard) is the analytical standard of Niflumic acid. This product is intended for research and analytical applications. Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-A0012R
-
|
UK-88525 (hydrobromide) (Standard)
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-B0596
-
|
TA-0910
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-152293
-
|
|
VEGFR
ERK
|
Cancer
|
|
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W010201
-
|
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-112296
-
T025
2 Publications Verification
|
CDK
Apoptosis
DYRK
|
Cancer
|
|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
|
-
- HY-150605
-
|
|
ERK
|
Cancer
|
|
ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC50 of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC50 of 31 nM .
|
-
- HY-163796
-
-
- HY-12279
-
|
TGR-1202; RP5264
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
|
-
- HY-114245R
-
-
- HY-114245B
-
|
Methylselenocysteine hydrochloride; Se-Methylseleno-L-cysteine hydrochloride
|
Endogenous Metabolite
Apoptosis
Beta-secretase
|
Cancer
|
|
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis .
|
-
- HY-114245
-
|
Methylselenocysteine; Se-Methylseleno-L-cysteine
|
Apoptosis
Endogenous Metabolite
Beta-secretase
|
Cancer
|
|
Se-Methylselenocysteine, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine is orally bioavailable, and induces apoptosis .
|
-
- HY-12279B
-
|
TGR-1202 sulfate; RP-5264 sulfate
|
PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .
|
-
- HY-163795
-
|
|
EBI2/GPR183
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
GPR183-IN-1 (compound 15) is a potent and orally activity GPR183 inhibitor. GPR183-IN-1 inhibits Ca 2+ mobilization with an IC50 value of 39.97 nM. GPR183-IN-1 has the potential for the research of cancer, autoimmune diseases, pain, and osteoporosis .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-19896
-
COTI-2
2 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
|
-
- HY-N0234R
-
|
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
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- HY-B0239S2
-
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JNK
Apoptosis
VEGFR
MMP
Bacterial
Akt
Autophagy
HIF/HIF Prolyl-Hydroxylase
Antibiotic
Beclin1
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Cancer
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Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
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- HY-12169
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BB2516; TA2516
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MMP
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Cancer
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Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes .
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- HY-N6985
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Others
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Cancer
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Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment[1][2].
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- HY-W010201R
-
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(±)-Citronellol (Standard); (±)-β-Citronellol (Standard)
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Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
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Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
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- HY-164530
-
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Src
VEGFR
Raf
p38 MAPK
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Cancer
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SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
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- HY-B0596A
-
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TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
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Neurological Disease
Endocrinology
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Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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- HY-164445
-
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STAT
|
Cancer
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STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
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- HY-101448
-
|
WAY-171318
|
MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
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- HY-159510
-
|
|
Apoptosis
VEGFR
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
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VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrial membrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
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- HY-N6871
-
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Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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- HY-150652
-
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FGFR
Apoptosis
|
Cancer
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FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
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- HY-145260
-
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Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
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BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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- HY-168081
-
|
|
PD-1/PD-L1
|
Cancer
|
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PD-1/PD-L1-IN-52 (Compound III-5) is an orally active PD-1/PD-L1 inhibitor that blocks the interaction between PD-1 and PD-L1, with an IC50 of 109.9 nM. PD-1/PD-L1-IN-52 exhibits antitumor activity in a C57BL/6 mouse xenograft model implanted with human PD-1-expressing MC38 colon cancer cells, with a TGI of 49.6% .
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-
- HY-12678S1
-
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NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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-
- HY-P10424
-
|
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PD-1/PD-L1
|
Cancer
|
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OPBP-1 is a D-peptide obtained by phage display screening, molecular docking and molecular dynamics simulation. OPBP-1 has high stability and strong antitumor and oral activity. OPBP-1 can selectively bind PD-L1 protein, significantly block the interaction between PD-1 and PD-L1, and this blocking effect helps to restore and improve the function of T lymphocytes and reduce the proportion of bone marrow derived suppressor cells (MDSCs) to combat tumor-induced immune escape. OPBP-1 can be used in cancer immunotherapy research .
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-
- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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- HY-10116
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
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- HY-164503
-
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NEP010
|
EGFR
|
Cancer
|
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Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR wt, EGFR L858R/T790M, EGFR L858R and EGFR T790M, respectively .
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- HY-161887
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
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-
- HY-173060
-
|
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ERK
Apoptosis
Autophagy
|
Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
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- HY-N0330
-
|
|
Apoptosis
Autophagy
PI3K
c-Myc
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity .
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-
- HY-149401
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
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-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
|
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
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-
- HY-139920A
-
|
SH-1028 mesylate
|
EGFR
|
Cancer
|
|
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
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-
- HY-168851
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-35 (compound T26) is a selective, orally active, cross -the blood-brain barrierPARP1 inhibitor with IC50 values of 0.2, 122 nM for PARP1, PARP2, respectively. PARP1-IN-35 shows antiproliferative activity and anticancer activity. PARP1-IN-35 has the potential for the research of breast cancer .
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-
- HY-N0281
-
|
7,8-Dihydroxycoumarin
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1?, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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-
- HY-150609
-
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SHP2
Phosphatase
CDK
|
Cancer
|
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
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-
- HY-151137
-
|
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mTOR
HSP
Apoptosis
Autophagy
|
Cancer
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|
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .
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-
- HY-111458
-
|
|
Deubiquitinase
|
Cancer
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GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
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-
- HY-164529
-
|
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Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
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-
- HY-15898
-
Y-320
3 Publications Verification
|
Interleukin Related
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer .
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-
- HY-N0330R
-
|
|
Apoptosis
Autophagy
PI3K
c-Myc
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Momordin Ic (Standard) is the analytical standard of Momordin Ic. This product is intended for research and analytical applications. Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity .
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-
- HY-168555
-
|
|
CDK
PROTACs
Apoptosis
|
Cancer
|
|
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
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-
- HY-149493
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
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-
- HY-145925B
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor) .
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-
- HY-159912
-
|
|
YAP
|
Cancer
|
|
pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
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-
- HY-N0281R
-
|
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
|
Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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-
- HY-16475
-
|
|
Hedgehog
|
Cancer
|
|
TAK-441 is a highly potent and orally active hedgehog (Hh) signaling inhibitor with an IC50value of 4.4 nM. TAK-441 has strong antitumor activity in solid tumors .
|
-
- HY-143445
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
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-
- HY-168954
-
|
|
c-Fms
Apoptosis
Akt
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .
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-
- HY-159905
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy .
|
-
- HY-135748A
-
|
|
Toll-like Receptor (TLR)
Apoptosis
|
Infection
Cancer
|
|
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
|
-
- HY-112608
-
|
|
PI3K
|
Cancer
|
|
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
|
-
- HY-19357
-
-
| Cat. No. |
Product Name |
Type |
-
- HY-B0497G
-
|
BAY2353 (GMP)
|
Fluorescent Dye
|
|
Niclosamide (GMP) is Niclosamide (HY-B0497) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-10585AG
-
|
Sodium Valproate (sodium) (GMP)
|
Fluorescent Dye
|
|
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-14397G
-
|
Indometacin (GMP)
|
Fluorescent Dye
|
|
Indomethacin (GMP) is Indomethacin (HY-14397) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research .
|
| Cat. No. |
Product Name |
Type |
-
- HY-P3161
-
|
|
Native Proteins
|
|
Lactoferrin from Bovine milk is a substance released by neutrophils. Lactoferrin from Bovine milk is an orally active multifunctional iron binding glycoprotein. Lactoferrin from Bovine milk prevents cell adhesion, growth and spreading of cell colonies. Lactoferrin from Bovine milk also has antiviral activity and inhibits microbial and viral adhesion and entry into host cells. Besides, Lactoferrin from Bovine milk has anti-inflammatory, immunomodulatory, and anti-cancer activities .
|
-
- HY-D0848
-
|
Bisacrylamide; MBA; Methylenebisacrylamide; N,N-Methylenebisacrylamide
|
Thickeners
|
|
N,N'-Methylenebisacrylamide (Bisacrylamide) is an orally active acrylamide dimer and crosslinker. N,N'-Methylenebisacrylamide increases CYP2E1, P53, cleaved caspase-3. N,N'-Methylenebisacrylamide promotes hepatic cancer. N,N'-Methylenebisacrylamide changes sperm abnormality rate and sperm count. N,N'-Methylenebisacrylamide decreases the number of various cells in the blood as well as induces liver and testicular damage. N,N'-Methylenebisacrylamide is used to prepare polyacrylamide gel .
|
-
- HY-B0497G
-
|
BAY2353 (GMP)
|
Biochemical Assay Reagents
|
|
Niclosamide (GMP) is Niclosamide (HY-B0497) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-10585AG
-
|
Sodium Valproate (sodium) (GMP)
|
Biochemical Assay Reagents
|
|
Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches .
|
-
- HY-14397G
-
|
Indometacin (GMP)
|
Biochemical Assay Reagents
|
|
Indomethacin (GMP) is Indomethacin (HY-14397) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Indomethacin (Indometacin) is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin has anticancer activity and anti-infective activity. Indomethacin can be used for cancer, inflammation and viral infection research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-156002
-
|
Paluratide
|
Ras
ERK
|
Cancer
|
|
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
|
-
- HY-W011258
-
|
L-Tyrosyl-L-phenylalanine
|
Xanthine Oxidase
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cancer
|
|
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells .
|
-
- HY-P5557
-
|
|
Bacterial
Necroptosis
|
Cancer
|
|
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells .
|
-
- HY-P2385
-
-
- HY-P10424
-
|
|
PD-1/PD-L1
|
Cancer
|
|
OPBP-1 is a D-peptide obtained by phage display screening, molecular docking and molecular dynamics simulation. OPBP-1 has high stability and strong antitumor and oral activity. OPBP-1 can selectively bind PD-L1 protein, significantly block the interaction between PD-1 and PD-L1, and this blocking effect helps to restore and improve the function of T lymphocytes and reduce the proportion of bone marrow derived suppressor cells (MDSCs) to combat tumor-induced immune escape. OPBP-1 can be used in cancer immunotherapy research .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N6642
-
-
-
- HY-N2486
-
-
-
- HY-N0410
-
-
-
- HY-N0203
-
-
-
- HY-N1486
-
-
-
- HY-N0015
-
-
-
- HY-N0451
-
-
-
- HY-N11644
-
-
-
- HY-N0410R
-
-
-
- HY-34544R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Others
|
|
Daucosterol (Standard) is the analytical standard of Daucosterol. This product is intended for research and analytical applications. Daucosterol is an orally active natural sterol compound, which has anti-inflammatory, anticancer and immunomodulatory activities. Daucosterol inhibits cancer cell proliferation by inducing autophagy through ROS-dependent manner. Daucosterol also inhibits colon cancer growth by inducing apoptosis, inhibiting cell migration and invasion and targeting caspase signalling pathway .
|
-
-
- HY-N3665
-
-
-
- HY-N7640
-
-
-
- HY-W005130
-
-
-
- HY-N2486R
-
-
-
- HY-N12960
-
-
-
- HY-N0256
-
-
-
- HY-17363
-
-
-
- HY-N2510
-
-
-
- HY-17473
-
-
-
- HY-N7083
-
-
-
- HY-N7271
-
-
-
- HY-N1261
-
-
-
- HY-N2959
-
-
-
- HY-N11536
-
-
-
- HY-W011641
-
-
-
- HY-N0451R
-
-
-
- HY-N2342
-
-
-
- HY-N0203R
-
-
-
- HY-N6257
-
-
-
- HY-17583
-
-
-
- HY-119906
-
-
-
- HY-N0256R
-
|
|
Triterpenes
Structural Classification
Hedera nepalensis K. Koch var. sinensis (Tobl.) Rehd.
Terpenoids
Source classification
Plants
Araliaceae
|
COX
NF-κB
|
|
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
|
-
-
- HY-113327R
-
|
|
Natural Products
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
|
Drug Metabolite
Endogenous Metabolite
|
|
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
|
-
-
- HY-N6996
-
-
-
- HY-N1109
-
-
-
- HY-N2510R
-
-
-
- HY-N0015R
-
-
-
- HY-W403933R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Autophagy
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
-
- HY-17363R
-
-
-
- HY-17473R
-
|
|
Quinones
Structural Classification
Source classification
Benzene Quinones
Embelia laeta (Linn.) Mez
Plants
Myrsinaceae
|
IAP
NF-κB
Apoptosis
Autophagy
|
|
Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
-
- HY-N2420
-
-
-
- HY-Y0966
-
-
-
- HY-N6884
-
-
-
- HY-N2959R
-
-
-
- HY-B0412
-
-
-
- HY-N7271R
-
-
-
- HY-B2163
-
-
-
- HY-16594
-
|
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Proteasome
Apoptosis
ROS Kinase
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
-
- HY-W012241R
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Endogenous Metabolite
|
|
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
-
- HY-10585
-
-
- HY-N7083R
-
-
- HY-N6257R
-
-
- HY-N7140
-
-
- HY-N2342R
-
-
- HY-10585A
-
-
- HY-N6954
-
-
- HY-N6884R
-
|
|
Bixaceae
Bixa orellana Linn.
Ketones, Aldehydes, Acids
Source classification
Plants
|
Reactive Oxygen Species
Apoptosis
|
|
Bixin (Standard) is the analytical standard of Bixin. This product is intended for research and analytical applications. Bixin, isolated from the seeds of Bixa orellana, is an orally active carotenoid. Bixin induces apoptosis in cancer cells. Bixin possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation.
|
-
- HY-121619
-
-
- HY-N2181
-
|
|
Quinones
Structural Classification
Classification of Application Fields
Source classification
Phenols
Polyphenols
Plants
Lithospermum erythrorhizon Sieb. et Zucc.
Naphthalene Quinones
Boraginaceae
Inflammation/Immunology
Disease Research Fields
|
Cytochrome P450
Apoptosis
Bacterial
Autophagy
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
|
-
- HY-N3248
-
-
- HY-10585B
-
-
- HY-12033
-
-
- HY-N3980
-
|
Champacol; Guaiac alcohol
|
Infection
Structural Classification
Natural Products
Classification of Application Fields
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
Disease Research Fields
|
Autophagy
RAD51
|
|
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-N6996R
-
-
- HY-Y0966R
-
-
- HY-B2163R
-
|
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
|
Astaxanthin (Standard) is the analytical standard of Astaxanthin. This product is intended for research and analytical applications. Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
|
-
- HY-10585AR
-
-
- HY-Y1117
-
-
- HY-N3980R
-
|
|
Structural Classification
Natural Products
Source classification
Distemonanthus benthamianus Baill.
Plants
Compositae
|
Autophagy
RAD51
|
|
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
|
-
- HY-B0367
-
-
- HY-114319
-
-
- HY-W015828
-
-
- HY-40161
-
-
- HY-120149
-
-
- HY-N6954R
-
|
|
Structural Classification
other families
Xanthones
Garcinia oblongifolia Champ. ex Benth.
Guttiferae
Source classification
Phenols
Polyphenols
Plants
|
ATM/ATR
STAT
CDK
Hedgehog
|
|
Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active .
|
-
- HY-117025A
-
-
- HY-117025
-
-
- HY-N0447
-
|
|
Zingiber officinale Roscoe
Structural Classification
Monophenols
Classification of Application Fields
Source classification
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Zingiberaceae
Cancer
|
TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
|
|
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
|
-
- HY-N0108
-
-
- HY-N6973
-
-
- HY-N0316
-
-
- HY-B1971
-
-
- HY-B1971R
-
-
- HY-B0239
-
-
- HY-N3945
-
|
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-N0316R
-
-
- HY-N6866
-
|
|
Structural Classification
Neurological Disease
Classification of Application Fields
Source classification
Lignans
Phenylpropanoids
Plants
Schisandraceae
Schisandra chinensis (Turcz.) Baill.
Inflammation/Immunology
Disease Research Fields
Cancer
|
Apoptosis
AMPK
Akt
PERK
Keap1-Nrf2
Caspase
PARP
GSK-3
NO Synthase
Interleukin Related
|
|
Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease .
|
-
- HY-N0234
-
-
- HY-16637D
-
-
- HY-B0239R
-
-
- HY-N0704
-
-
- HY-W010201
-
-
- HY-114245R
-
-
- HY-114245B
-
-
- HY-114245
-
-
- HY-N0234R
-
-
- HY-N6985
-
-
- HY-W010201R
-
-
- HY-N6871
-
|
|
Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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- HY-N0330
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- HY-138071
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- HY-N0281
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7,8-Dihydroxycoumarin
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Structural Classification
Daphne
Classification of Application Fields
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
Disease Research Fields
Cancer
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EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
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Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1?, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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- HY-N0330R
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Kochia scoparia L. Schrad.
Triterpenes
Structural Classification
Terpenoids
Source classification
Plants
Chenopodiaceae
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Apoptosis
Autophagy
PI3K
c-Myc
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Momordin Ic (Standard) is the analytical standard of Momordin Ic. This product is intended for research and analytical applications. Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity .
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- HY-N0281R
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Structural Classification
Daphne
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
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EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
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Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W654305
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Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
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- HY-17363S1
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Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate[1]. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research[2][3].
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- HY-142283BS
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N-Desmethyl dosimertinib-d5 is the deuterium labeled Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
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- HY-142283CS
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N-Methyl-dosimertinib-d5 is the deuterium labeled of Dosimertinib (HY-142283). Dosimertinib is a highly potent, selective, and orally active deuterated EGFR inhibiotor. Dosimertinib can be used for the research of non-small-cell lung cancer[1][2].
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- HY-B0497BS
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Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate[1]. Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research[2]. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells[5]. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells[3][4][6].
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- HY-N0565AS
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Doxycycline-d3 hydrochloride is deuterium labeled Doxycycline (hydrochloride). Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity .
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- HY-N0565S3
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Doxycycline- 13C,d3 is 13C and deuterium labeled Doxycycline. Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor . Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity .
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- HY-19822S2
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Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
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- HY-W703549
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Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
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- HY-B0497S2
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Niclosamide-d3 (BAY2353-d3) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
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- HY-78131S2
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Ibuprofen-d4 is a deuterium labeled Ibuprofen (HY-78131). Ibuprofen is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
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- HY-A0077S2
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Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine . Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation .
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- HY-78131CS
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1 Publications Verification
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Ibuprofen-d3 ((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
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- HY-168968S
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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- HY-170905S
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MAT2A-IN-22 (Compound 29-1) is a BBB-penatrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
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- HY-142283AS
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Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
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- HY-78131S3
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Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers .
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- HY-19939S
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4 Publications Verification
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VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
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- HY-19822S3
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Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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- HY-B0520AS1
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Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
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- HY-109523S
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Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-19822S
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Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
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- HY-B0520AS
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Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
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- HY-15306S
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1 Publications Verification
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Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
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- HY-12033S2
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2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
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- HY-12033S
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2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
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- HY-12033S1
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2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
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- HY-142283
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Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
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- HY-114277S
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Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
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- HY-114277S2
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Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
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- HY-10409S
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Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
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- HY-12678S
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Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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- HY-B0239S2
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Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol[1]. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research[2][3][4].
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- HY-12678S1
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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| Cat. No. |
Product Name |
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Classification |
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- HY-135699
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TD52
1 Publications Verification
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Alkynes
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TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-135699A
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Alkynes
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TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-162356
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Azide
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PD-L1-IN-4 (Compound X18) is an orally active PD-L1 inhibitor that exhibits remarkable inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
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Product Name |
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Classification |
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- HY-Y0966
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Fillers
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Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
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