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Cat. No. Product Name CAS No. Information
PC-63391

ASTX660

1799328-86-1

ASTX660 is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

Blood Cancer

Phase 2 Clinical

PC-45289

Embelin

550-24-3

Embelin (Embelic acid, Emberine, NSC-91874) is a cell-permeable benzoquinone compound that exhibits antitumor properties; specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50=4.1 uM); has anti-inflammatory activities in both acute and chronic irritant contact dermatitis in vivo; also inhibits plasminogen activator inhibitor-1 (PAI-1) with IC50 of 1.62 uM.

PC-35081

MX107

2170102-50-6 MX107 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 3.1 uM; significantly enhances the tumoricidal efficacy of doxorubicin in TNBC cells, induces degradation of XIAP and/or cIAP1, which inhibited NF-κB activation by genotoxic agents.
PC-35080

MX106

2170836-81-2 MX106 is a novel potent survivin inhibitor, effectively suppresses MDA-MB-231 cells proliferation with IC50 of 2.2 uM; significantly enhances the tumoricidal efficacy of doxorubicin in TNBC cells, induces degradation of XIAP and/or cIAP1, which inhibited NF-κB activation by genotoxic agents.
PC-63393

ASTX660 mesylate

1799328-90-7 ASTX660 mesylate is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

Blood Cancer

Phase 2 Clinical

PC-63392

ASTX660 hydrochloride

1799328-50-9 ASTX660 hydrochloride is a novel potent IAP antagonist that targets the BIR3 domain of cIAP1/2 and XIAP with IC50 of 12 nM and <40 nM; potently inhibits association between XIAP and caspase 9 in HEK293 cell line with EC50 of 2.8 nM, binds to and leads to the degradation of cIAP1/2 and stabilisation of NIK in cell; induces apoptosis in MDA-MB-231 cells with EC50 of 1.8 nM, which is TNF-α-dependent; inhibits tumor growth in mice bearing breast and melanoma tumor xenografts.

Blood Cancer

Phase 2 Clinical

PC-43254

UC-112

383392-66-3 UC-112 is a novel IAP inhibitor that potently inhibits human melanoma (A375 and M14) and human prostate (PC-3 and DU145) cancer cell lines with IC50 of 0.7-3.4 uM; also potently inhibits the growth of P-gp-overexpressed multidrug-resistant cancer cells, strongly activates caspase-3/7 and caspase-9 activities, and selectively downregulates survivin level at 1 uM; strongly inhibits tumor growth and reduces both X chromosome-linked IAP and survivin levels in an A375 human melanoma xenograft model in vivo.

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