CAS NO. |
Products Name |
1799633-27-4 |
S-63845 |
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S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor; binds human MCL1 with a Kd of 0.19 nM. |
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1025504-45-3 |
Valbenazine |
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Valbenazine is a prodrug of the (+)-α isomer of tetrabenazine for tardive syndrome therapy, and inhibits VMAT2 function. |
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1629869-44-8 |
Pimodivir |
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Pimodivir is an orally bioavailable inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit. |
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1703793-34-3 |
BLU285 |
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Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V. |
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871361-88-5 |
SC66 |
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SC66 is a novel AKT inhibitor, IC50 values of approximately 0.75 μg/ml at 72 hours in HepG2, HA22T/VGH and PLC/PRF/5 cells. IC50 value: 0.75 μg/ml (72 hours in HepG2, HA22T/VGH and PLC/PRF/5 cells) [1] Target: Akt in vitro: Each cell line had a different sensitivity to SC66, as evidenced by the IC50 values . HepG2, HA22T/VGH and PLC/PRF/5 cells had similar IC50 values of approximately 0.85 and 0.75 μg/ml at 48 and 72 hours, respectively. The most resistant cell line was Huh7, which showed an IC50 of 3.1 and 2.8 μg/ml at 48 and 72 hours respectively, while the Hep3B cell line was found to be the most sensitive, with an IC50 of 0.75 and 0.5 μg/ml at 48 and 72 hours, respectively. SC66 reducew cell viability in a dose- and time-dependent manner, inhibited colony formation and induced apoptosis in HCC cells. SC66 treatment led to a reduction in total and phospho-AKT levels. In addition, SC66 induces the production of reactive oxygen species (ROS) and DNA damage. SC66 significantly potentiates the effects of both conventional chemotherapeutic and targeted agents, doxorubicin and everolimus, respectively. [1] SC66 manifests a more effective growth suppression of transformed cells compared with other inhibitors of PIP3/Akt pathway. SC66 represents a unique chemical tool to investigate the mechanisms of ubiquitination-dependent Akt regulation in physiological and stressed conditions. SC66 directly facilitates Akt ubiquitination. [2] In vivo: SC66 inhibits tumor growth of Hep3B cells in xenograft models. [1] |
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1802220-02-5 |
TPX-0005 |
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TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively. |
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1693731-40-6 |
CCT251236 |
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CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction |
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944328-88-5 |
QS11 |
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QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. |
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900185-02-6 |
PIK294 |
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PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, less potent to PI3Kα/β/γ. IC50 value: 10 nM(p110δ) [1] Target: p110δ inhibitor PIK-294 shows distinct patterns of isoform selectivity to inhibit different subsets of class I PI3K isoforms (p110β, p110δ, and p110γ) and exhibits low sensitivity to p110α with IC50 of 10 μM). The m-phenol moiety of PIK-294 is able to penetrate the deep-affinity pocket of the ATP binding site, and thus increases in vitro inhibitory activity |
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380899-24-1 |
SB649868 |
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SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively). |
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