Search Result
Results for "
B cell inhibition
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-16399
-
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Apoptosis
SF3B1
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Cancer
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Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis .
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- HY-N3001
-
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STAT
VEGFR
Bcl-2 Family
Survivin
IAP
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Cancer
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Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells . Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
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-
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- HY-108431
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Apoptosis
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Cancer
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MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity .
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-
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- HY-33299
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BTCA
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Biochemical Assay Reagents
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Cancer
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Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
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- HY-125762
-
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Tyrosinase
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Cancer
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Tyrosinase-IN-16 (compound 19a) is a tyrosine kinase (Tyrosinase) inhibitor with Ki=470 nM. Tyrosinase-IN-16 is cytotoxic to B16F10 cells, with >90% inhibition at 20 μM .
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-
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- HY-125376
-
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PI3K
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Cancer
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PI3Kδ-IN-3 (Compound 11) is a PI3Kδ inhibitor (IC50: 9 nM). PI3Kδ-IN-3 inhibits B cell function. PI3Kδ-IN-3 has good pharmacokinetic properties .
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-
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- HY-N8304
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(+)-Shegansu B; Parvifolol D
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Interleukin Related
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Inflammation/Immunology
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Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity .
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- HY-167853
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SK-1080
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Angiotensin Receptor
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Metabolic Disease
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KR-31080 is an derivative of imidazo [4,5-b] pyridine. KR-31080 inhibits angiotensin II receptor. KR-31080 inhibits the NO production in LPS-stimulated BV-2 cells at a concentration of 2 μm with inhibition of 8.3% .
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-
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- HY-125629
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Others
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Others
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Primordazine B is a small molecule compound identified by chemical screening in zebrafish embryos with the activity of selectively destroying Primordial Germ Cells (PGCs). Primordazine B inhibits a process called Poly(A)-tail Independent Non-canonical Translation (PAINT) without inhibition of polyadenylate tail dependent typical translation (PAT). Primordazine B can be used to study translational control of cells in specific physiological or pathological states, such as gene expression regulation during cell dormancy, viral infection, or stress conditions .
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- HY-121998
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Aurora Kinase
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Others
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Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
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- HY-N10649
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Phosphatase
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Metabolic Disease
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PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
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- HY-N10648
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Phosphatase
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Metabolic Disease
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PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
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- HY-147091
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Ligands for Target Protein for PROTAC
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Cancer
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Tazemetostat de(methyl morpholine)-COOH (compound 7) is a ligand for the PROTAC target protein EZH2, which can be used to synthesis of EZH2 degraders (PROTACs). EZH2 degraders have potent cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphoma .
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- HY-169400
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HDAC
Histone Methyltransferase
Apoptosis
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Cancer
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HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
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- HY-W013274
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CPTH2
1 Publications Verification
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Histone Acetyltransferase
Apoptosis
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Cancer
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CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .
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- HY-W013274A
-
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Histone Acetyltransferase
Apoptosis
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Cancer
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CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B) .
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- HY-114585
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Bacterial
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Infection
Cancer
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Sperabillin A is an antibacterial agent against gram-positive and gram-negative bacteria. Sperabillin A shows strong inhibition of human umbilical vein endothelial (HUVE) cell proliferation. Sperabillin A also shows anti-tumor acfivity against B16 melanoma in mouse .
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- HY-100866B
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Bcl-2 Family
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Cancer
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F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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- HY-100866
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Bcl-2 Family
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Cancer
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F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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- HY-B0199
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RS 61443; TM-MMF
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Drug Metabolite
Apoptosis
Endogenous Metabolite
Bacterial
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Cancer
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Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .
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- HY-160682
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EGFR
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Others
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EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
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- HY-100866A
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Bcl-2 Family
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Cancer
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F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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- HY-N3239
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NADPH Oxidase
HBV
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Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress . Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with IC50 of 3.99 μM .
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- HY-129388A
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CC-90011; LSD1-IN-7
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Histone Demethylase
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Cancer
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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-B0563BS
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Isotope-Labeled Compounds
Potassium Channel
Sodium Channel
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Neurological Disease
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Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
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- HY-129388B
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CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
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Histone Demethylase
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Cancer
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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 .
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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-19542
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C6-Cer; N-Hexanoylsphingosine
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Apoptosis
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Cancer
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C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-N10760
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Others
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Metabolic Disease
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2a,3a,23-Trihydroxyurs-12,20(30)-dien-28-oic acid (compound 3), a triterpenoid, significantly decreases the level of fibronectin in High-Glucose and TGF-b1 induced HK-2 cells with 27.66 % inhibition rate at 10 μM .
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- HY-119702
-
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HBV
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Infection
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YZ51 is a derivative of Osalmid (HY-B2116) with stronger ribonucleotide reductase (RR) inhibitory activity and HBV replication inhibition ability than Osalmid. The IC50 of YZ51 against recombinant RR activity is 0.6 μM, and the IC50 against HepG2.2.15 cell RR activity is 23.7 μM .
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- HY-165484
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Interleukin Related
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Inflammation/Immunology
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AVP-13358 is an orally active IgE inhibitor that effectively suppresses immunoglobulin E (IgE)-mediated immune responses, with IC50 values of 8 and 3 nM for IgE inhibition in vivo and in vitro in BALB/c mice, respectively. AVP-13358 acts directly on T cells, inhibiting the production and release of IL-4, IL-5, and IL-13. It also targets other markers critical for the development of allergic responses, including the B cell IgE receptor (CD23) in human monocytes and the CD23 and IL-4 receptors in mouse B cells. AVP-13358 can be used in research related to anti-allergic responses .
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- HY-129388
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CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
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Histone Demethylase
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Cancer
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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 .
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- HY-B0987
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L-Ascorbic acid 6-hexadecanoate; 6-O-Palmitoyl-L-ascorbic acid
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Reactive Oxygen Species
Endogenous Metabolite
Calcium Channel
Sodium Channel
Apoptosis
NOD-like Receptor (NLR)
Bcl-2 Family
Caspase
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Inflammation/Immunology
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Ascorbyl palmitate is an orally active ester formed from ascorbic acid and palmitic acid, used as an antioxidant and food additive. Ascorbyl palmitate in preventing fat and oil oxidation is more efficient than Butylated hydroxyanisole (HY-B1066) and Butylated hydroxytoluene (HY-Y0172). Ascorbyl palmitate mitigates inhibition of collagen synthesis by select calcium and sodium channel blockers. Ascorbyl palmitate induces Apoptosis in human umbilical vein endothelial cells (HUVECs). Ascorbyl palmitate ameliorates inflammatory diseases by inhibition of NLRP3 inflammasome .
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- HY-163272
-
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Glutathione Peroxidase
CDK
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Cancer
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GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC50 values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo .
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- HY-164702
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Antibody-Drug Conjugates (ADCs)
EGFR
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Cancer
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BL-B01D1 is a bispecific ADC, which targets EGFR and HER3 through bispecific antibody Izalontamab (HY-P99676), and exhibits cytotoxicity against various cancer cells via inhibition of DNA replication and DNA synthesis by its ADC toxin ED04 (HY-153891) .
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- HY-106963
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LGD1550
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RAR/RXR
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Cancer
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ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
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- HY-B0199S
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Isotope-Labeled Compounds
Drug Metabolite
Apoptosis
Endogenous Metabolite
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Cancer
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Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation[1].
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- HY-121138
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ARDP0006; DHDNE
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Flavivirus
Dengue virus
Virus Protease
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Infection
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1,8-Dihydroxy-4,5-dinitroanthraquinone (ARDP0006; DHDNE) is a potent inhibitor of serine proteinase NS2B/3, the dengue viral protein. 1,8-Dihydroxy-4,5-dinitroanthraquinone has intermolecular proteinase activity and viral inhibition ability with IC50s of 432 μM and 4.2 μM, respectively. Meanwhile 1,8-Dihydroxy-4,5-dinitroanthraquinone inhibits NS2B/3 cleavage in BHK-21 cells at a dose ranging from 4.2 μM to 432 μM .
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- HY-18957C
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BGB-283 hydrochloride
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Endogenous Metabolite
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Cancer
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Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
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- HY-B0199R
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RS 61443 (Standard); TM-MMF (Standard)
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Drug Metabolite
Apoptosis
Endogenous Metabolite
Bacterial
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Cancer
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Mycophenolate Mofetil (Standard) is the analytical standard of Mycophenolate Mofetil. This product is intended for research and analytical applications. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .
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-
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- HY-164002
-
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Btk
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Others
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PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .
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- HY-143487
-
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Parasite
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Infection
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Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli .
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- HY-N7085
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5,7-Dimethoxycoumarin; Limettin
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JNK
p38 MAPK
ERK
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Neurological Disease
Inflammation/Immunology
Cancer
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Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
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- HY-B0439S1
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Sulphadoxine d3
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Parasite
Antibiotic
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Infection
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Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
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- HY-120323
-
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TNF Receptor
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Inflammation/Immunology
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DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively .
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- HY-162873
-
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MEK
Raf
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Cancer
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MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
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- HY-111101
-
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IRAK
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Cancer
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AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL) .
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- HY-149838
-
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NF-κB
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Cancer
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NF-κB-IN-9 is a nuclear factor kappa B (NF-κB) targeting sonosensitizer (λex/λem=489/628 nm). NF-κB-IN-9 exhibits strong inhibition on NF-κB signaling due to its two resveratrol units in one molecule. NF-κB-IN-9 has anti-tumor activity and shows remarkable sonocytotoxicity against cancer cells. NF-κB-IN-9 has biosafety in eenograft mice model.
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- HY-W699318
-
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Reactive Oxygen Species
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Others
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1-Oleoyl-2-palmitoylglycerol is a diacylglycerol in which an oleic acid and a palmitic acid are attached to sn-1 and sn-2 position. 1-Oleoyl-2-palmitoylglycerol enhances the inhibition of superoxide anion production induced by fMLF/cytochalasin B (CB) in human neutrophils. 1-Oleoyl-2-palmitoylglycerol can be used in research about lipid metabolism, membrane fluidity, or the distribution and function of lipids in cells .
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- HY-158138
-
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PARP
Topoisomerase
Apoptosis
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Cancer
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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% .
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- HY-N7085R
-
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ERK
JNK
p38 MAPK
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Neurological Disease
Inflammation/Immunology
Cancer
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Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
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- HY-116633
-
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Endogenous Metabolite
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Infection
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BCM-599 is a HBV (hepatitis B virus) capsid assembly inhibitor with the activity of inhibiting HBV capsid assembly. BCM-599 showed an IC50 value of 0.88μM and a CC50 value of 144μM in HepG2.2.15 cells. When used in combination with lamivudine, BCM-599 showed a synergistic inhibitory effect on viral concentration. BCM-599 can be used as an effective combined inhibition option for HBV infection .
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- HY-168551
-
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PROTACs
Anaplastic lymphoma kinase (ALK)
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Cancer
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PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC50 is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)) .
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- HY-161641
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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- HY-119293
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K777
1 Publications Verification
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Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
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Infection
Cancer
|
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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- HY-119293A
-
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Cathepsin
CCR
Cytochrome P450
Parasite
SARS-CoV
Filovirus
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Infection
Cancer
|
K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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-
- HY-138074
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5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
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Parasite
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Infection
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Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
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- HY-153321
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BTK-IN-24
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Btk
PROTACs
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Inflammation/Immunology
Cancer
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NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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- HY-14909
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Bardoxolone
Maximum Cited Publications
17 Publications Verification
CDDO; RTA 401
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Keap1-Nrf2
Necroptosis
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Metabolic Disease
Cancer
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Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease .
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- HY-150563
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Monoamine Oxidase
Amyloid-β
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Neurological Disease
Inflammation/Immunology
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Neuroinflammatory-IN-2 is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease .
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- HY-N6871
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Bacterial
IKK
Ferroptosis
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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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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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-100866B
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Bcl-2 Family
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Cancer
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F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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- HY-100866
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Bcl-2 Family
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Cancer
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F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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- HY-100866A
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Bcl-2 Family
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Cancer
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F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99279
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Anti-Human Phosphatidylserine Recombinant Antibody
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Inhibitory Antibodies
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Cancer
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Bavituximab (Anti-Human Phosphatidylserine Recombinant Antibody) is a phosphatidylserine (PS)-targeting monoclonal antibody, suppresses tumor growth by targeting tumor vasculature and reactivating antitumor immunity. Bavituximab plus Paclitaxel (HY-B0015) and Carboplatin (HY-17393), have enhanced inhibition on non-small-cell lung cancer .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N3001
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- HY-B0199
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- HY-N3239
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- HY-B0987
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- HY-N8304
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- HY-N10649
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- HY-N10648
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- HY-114585
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- HY-N10760
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- HY-B0199R
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- HY-N7085
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- HY-N7085R
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Structural Classification
Natural Products
Rutaceae
Plants
Citrus medica Linn. var. sarcodactylis (Noot.) Swingle
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ERK
JNK
p38 MAPK
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Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
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- HY-N6871
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Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
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Bacterial
IKK
Ferroptosis
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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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Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0199S
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Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation[1].
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- HY-B0439S1
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Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
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- HY-B0563BS
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Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
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