Search Result
Results for "
A375
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-128224
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Others
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Cancer
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Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC50 value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer .
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-
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- HY-161882
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PROTACs
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Cancer
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PROTAC SMARCA2 degrader-8 (compound 1) is a potent SMARCA2 degrader with a DC50 of 28nM in A375 cells .
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-
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- HY-N3838
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Others
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Cancer
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Epitulipinolide diepoxide (compound 9) is a natural compound isolated from the herbs of Liriodendron chinense (Hemsl.) Sarg. Epitulipinolide diepoxide displays cytoxicity in A375 cells, with the IC50 of 52.03 μM .
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-
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- HY-120607
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Parasite
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Infection
Cancer
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Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
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-
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- HY-120454
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MEK
Potassium Channel
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Cancer
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G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
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- HY-N10335
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FAK
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Inflammation/Immunology
Cancer
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Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
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- HY-158027
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Raf
VEGFR
FGFR
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Cancer
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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 .
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-
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- HY-153864
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PROTACs
MEK
ERK
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Cancer
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PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
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- HY-169086
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PROTACs
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Cancer
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KL-465 is a PROTAC degrader for MAGE-A3, that degrades MAGE-A3 with a DC50 of 2 μM in HeLa cell. KL-465 inhibits viability of MAGE-A3 positive cancer cell HCT116, A375 and HeLa. (Blue: Ligand for E3 ligase (HY-151227); Black: Linker (HY-W679862); Pink: Ligand for target protein (HY-169087))
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- HY-153445A
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MEK
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Cancer
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MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC50 of 2 nM for A375 cells .
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- HY-153469
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ADC Cytotoxin
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Cancer
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Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
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-
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- HY-N12834
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Others
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Inflammation/Immunology
Cancer
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Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
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- HY-144271
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Raf
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Cancer
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RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
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- HY-162900
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HSP
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Cancer
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HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC50 values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents .
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- HY-16667
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Early 2 Factor (E2F)
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Cancer
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HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
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-
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- HY-144269
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Raf
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Cancer
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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 .
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- HY-153738
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ERK
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Cancer
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ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
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- HY-122506
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STAT
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Cancer
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Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells .
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- HY-153341
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PROTACs
Raf
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Cancer
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CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ™) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. CFT1946 can be used in tumor research .
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- HY-13323
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DNA/RNA Synthesis
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Cancer
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CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-169298
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Ferroptosis
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Cancer
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Ferroptosis-IN-15 (compound 12) is a potent inhibitor of ferroptosis, with the EC50s of 0.76 and 0.67 μM in A375 cells and 786-O cells, respectively.Ferroptosis-IN-15 is a potential iron chelator and radical trapping antioxidant .
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- HY-13323A
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DNA/RNA Synthesis
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Cancer
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CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
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- HY-153445
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ERK
MEK
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Cancer
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MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
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- HY-N0201
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TNF Receptor
Toll-like Receptor (TLR)
JAK
STAT
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Cancer
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Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
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- HY-12842
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IAP
Apoptosis
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Cancer
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UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
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- HY-147788
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Dihydroorotate Dehydrogenase
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Cancer
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hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
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- HY-117872
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20-O-Acetylsartorypyrone D
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Fungal
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Infection
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Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
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- HY-15816A
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BVD-523 hydrochloride; VRT752271 hydrochloride
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ERK
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Cancer
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Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-15610
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RG 7421; MEK inhibitor 1
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MEK
Apoptosis
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Cancer
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GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
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- HY-147734
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Others
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Cancer
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Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
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- HY-13323R
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DNA/RNA Synthesis
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Cancer
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CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-15816
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BVD-523; VRT752271
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ERK
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Cancer
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Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-N0201R
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TNF Receptor
Toll-like Receptor (TLR)
JAK
STAT
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Cancer
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Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
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- HY-P1726A
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Melanocortin Receptor
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Cancer
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MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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- HY-161628
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Topoisomerase
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Cancer
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Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
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- HY-164474
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MEK
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Cancer
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DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
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- HY-117707
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Raf
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Cancer
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EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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- HY-138098
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Others
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Cancer
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Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
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- HY-121255
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(R)-Cryptopleurine; NSC 19912
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Others
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Cancer
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(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
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- HY-117991
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Others
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Cancer
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DW10075 is a novel, highly selective VEGFR inhibitor that targets the VEGF/VEGF receptor (VEGFR) pathway, which has been shown to be an effective anti-angiogenic approach for cancer therapy. Studies have found that DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3 among 21 kinases, while having no effect on the other 18 kinases, including FGFR and PDGFR. In human umbilical vein endothelial cells (HUVECs), DW10075 significantly prevented VEGF-induced activation of VEGFR and its downstream signaling, thereby inhibiting VEGF-induced HUVEC proliferation. In addition, DW10075 dose-dependently inhibited VEGF-induced HUVEC migration and tube formation, and suppressed angiogenesis in the rat aortic ring model and the chick embryo chorionic membrane model. DW10075 also exhibited antiproliferative activity against 22 different human cancer cell lines, with IC50 values ranging from 2.2 μmol/L (for U87-MG human glioblastoma cells) to 22.2 μmol/L (for A375 melanoma cells). In the nude mouse U87-MG xenograft tumor model, oral administration of DW10075 significantly inhibited tumor growth and reduced the expression of CD31 and Ki67 in tumor tissues. In summary, DW10075 is a potential anti-tumor angiogenesis agent that deserves further development.
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- HY-B0078
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Imidazole Carboxamide
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
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Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .
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- HY-126288
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ASTX029
4 Publications Verification
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ERK
Apoptosis
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Cancer
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ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity .
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- HY-162389
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Others
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Cancer
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Anticancer agent 202 (compound 3) is a Anticancer agent .
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- HY-B0078R
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Imidazole Carboxamide (Standard)
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Apoptosis
Nucleoside Antimetabolite/Analog
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Cancer
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Dacarbazine (Standard) is the analytical standard of Dacarbazine. This product is intended for research and analytical applications. Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .
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- HY-149005
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Histone Methyltransferase
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Cancer
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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 .
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- HY-147731
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HDAC
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Cancer
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HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .
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-
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- HY-148059
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B-Raf IN 10
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Raf
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Cancer
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Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity .
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-
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- HY-155571
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MDM-2/p53
IAP
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Cancer
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MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .
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- HY-163356
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-60 (BF3) is a tubulin polymerization inhibitor with anticancer activity. Tubulin polymerization-IN-60 (BF3) belongs to the colchicine binding site inhibitors (CBSIs) and disturbs cell cycle progression leading to G2/M arrest and apoptosis .
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- HY-B1139
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Apoptosis
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Neurological Disease
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Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .
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- HY-112089
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LXH254
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Raf
p38 MAPK
Bcr-Abl
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Cancer
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Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
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- HY-N4187
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- HY-117996
-
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CRM1
Apoptosis
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Cancer
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KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity .
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- HY-149616
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PROTACs
ERK
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Cancer
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PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
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- HY-157800
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TRX-E-009-1
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Microtubule/Tubulin
Apoptosis
PARP
Caspase
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Cancer
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Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity .
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- HY-B1139R
-
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Apoptosis
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Neurological Disease
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Tolperisone (hydrochloride) (Standard) is the analytical standard of Tolperisone (hydrochloride). This product is intended for research and analytical applications. Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .
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- HY-126214S
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DNA/RNA Synthesis
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Cancer
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JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
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- HY-12970A
-
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Histone Methyltransferase
Apoptosis
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Cancer
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EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer .
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- HY-N0351
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trans-4-Hydroxycinnamic acid
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Endogenous Metabolite
Bacterial
Apoptosis
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Inflammation/Immunology
Cancer
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p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
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- HY-12970
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Histone Methyltransferase
Apoptosis
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Cancer
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EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer .
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- HY-12847
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Raf
Src
Apoptosis
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Cancer
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CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
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- HY-143270
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- HY-137487
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PROTACs
Raf
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Cancer
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PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .
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- HY-155874
-
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CDK
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Cancer
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ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .
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- HY-N0351R
-
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Endogenous Metabolite
Bacterial
Apoptosis
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Inflammation/Immunology
Cancer
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p-Coumaric acid (Standard) is the analytical standard of p-Coumaric acid. This product is intended for research and analytical applications. p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
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- HY-129180
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PROTACs
CDK
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Cancer
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XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .
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- HY-144692
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MEK
PI3K
PERK
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Cancer
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MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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- HY-144693
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
- HY-146029
-
|
Apoptosis
|
Cancer
|
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .
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-
- HY-150591
-
|
Proteasome
|
Cancer
|
20S Proteasome-IN-3 is a 20S proteasome β5 subunit inhibitor (IC50=1.64 μM) . 20S Proteasome-IN-3 shows anti-tumor proliferation activity .
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-
- HY-147268
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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 .
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-
- HY-148174
-
|
DGK
|
Cancer
|
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
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-
- HY-149207
-
|
Tyrosinase
|
Metabolic Disease
|
Tyrosinase-IN-11 is a potent tyrosinase inhibitor with IC50s of 50 nM and 64 nM for L-tyrosinase and L-dopa, respectively. Tyrosinase-IN-11 has significant antioxidant activity and low cytotoxicity. Tyrosinase-IN-11 has the potential for skin hyperpigmentation research .
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-
- HY-153181
-
|
MEK
|
Cancer
|
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions .
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-
- HY-163595
-
|
Ras
|
Cancer
|
Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC50 of < 100 nM for KRAS G12D. Pan-RAS-IN-4 plays an important rile in cancer research .
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-
- HY-164039
-
|
Others
|
Cancer
|
Talorasib (compound 1-2) has antitumor activity .
|
-
- HY-B0150
-
Nicotinamide
Maximum Cited Publications
48 Publications Verification
Niacinamide; Nicotinic acid amide
|
Organoid
Endogenous Metabolite
Sirtuin
HBV
|
Cancer
|
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .
|
-
- HY-145702
-
|
MEK
ERK
|
Cancer
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-B0150A
-
Niacinamide Hydrochloride; Nicotinic acid amide Hydrochloride
|
Sirtuin
Endogenous Metabolite
HBV
|
Infection
Cancer
|
Nicotinamide Hydrochloride is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide Hydrochloride also inhibits SIRT1. Nicotinamide Hydrochloride increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibits tumor growth and improves survival. Nicotinamide Hydrochloride also has anti-HBV activity .
|
-
- HY-148070
-
|
FLT3
FAK
Cytochrome P450
|
Cancer
|
FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
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-
- HY-148713
-
|
Apoptosis
|
Cancer
|
Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces Apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity .
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-
- HY-157979
-
|
Aquaporin
|
Cancer
|
AQP3-IN-1 (compounds 3) is an AQP3 inhibitor with a IC50 value of 8.91 μM. AQP3-IN-1 inhibits cell proliferation of melanoma cells .
|
-
- HY-158023
-
-
- HY-160649
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo .
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-
- HY-N0202
-
Asterolide
|
ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-163858
-
|
Haspin Kinase
|
Cancer
|
Haspin-IN-4 (Compound 60) is a selective inhibitor of Haspin with an IC50 value of 0.01 nM. Haspin-IN-4 possesses anticancer activity and can be used in cancer research .
|
-
- HY-147356
-
|
DNA/RNA Synthesis
|
Cancer
|
ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 µM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays .
|
-
- HY-151799
-
|
p62
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
Antitumor agent-81 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. Antitumor agent-81 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
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-
- HY-P99115
-
ASC 22; KN 035
|
PD-1/PD-L1
|
Cancer
|
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25?nM. Envafolimab has the potential for the research of solid tumors .
|
-
- HY-151883
-
|
Apoptosis
MDM-2/p53
|
Cancer
|
APE1-IN-2 (compound AP1) is a Pt(IV) proagent, targeting a critical BER protein, apurinic/apyrimidinic endonuclease 1 (APE1). APE1-IN-2 shows anticancer activity. APE1-IN-2 induces intracellular accumulation of platinum and activates DNA damage response and apoptosis signals .
|
-
- HY-116107
-
|
Necroptosis
|
Cancer
|
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .
|
-
- HY-146276
-
|
HDAC
CDK
Apoptosis
|
Cancer
|
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
|
-
- HY-107767
-
DC 81
|
Antibiotic
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct .
|
-
- HY-118912
-
|
Others
|
Inflammation/Immunology
Cancer
|
BMH-9 (Compound Z54) is a modulator for nuclear receptor subfamily 2, group F, member 6 (NR2F6) (also known as nuclear orphan receptor Ear2) . BMH-9 is an activator for p53 signaling pathway through interaction with DNA. BMH-9 inhibits proliferation of human cancer cells, exhibits antitumor efficacy in NOD-SCID mouse models .
|
-
- HY-118119
-
|
PGE synthase
|
Cancer
|
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1726A
-
|
Melanocortin Receptor
|
Cancer
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99115
-
ASC 22; KN 035
|
PD-1/PD-L1
|
Cancer
|
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25?nM. Envafolimab has the potential for the research of solid tumors .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-126214S
-
|
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
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-
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