| Cat. No. |
Product Name |
CAS No. |
Information |
| GY02836 |
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. |
| GY05381 |
MV1
|
1001600-54-9 |
MV 1 is a small-molecule IAP antagonist that binds to select baculovirus IAP repeat (BIR) domains resulting in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs; induces cell death that is dependent on TNF signaling and de novo protein biosynthesis. |
| GY02318 |
AZD5582
|
1258392-53-8 |
AZD5582 is a dimeric Smac mimetic, potent IAP antagonist that binds potently to the BIR3 domains of cIAP1, cIAP2 and XIAP with IC50 of 15, 21and 15 nM, respectively; causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro; induces cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions in MDA-MB-231 xenograft-bearing mice. |
| GY02054 |
BV6
|
1001600-56-1 |
A small molecule, bivalent IAP antagonist that binds to the c-IAP1 and XIAP BIR2-BIR3 domains with Kd of 0.46 and 0.029 nM, respectively; results in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs; also induces induce TNFα-dependent cell death, exhibits single-agent cell killing activity in EVSA-T cell line (IC50=14 nM). |
| GY05232 |
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. |
| GY05231 |
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. |
| GY05341 |
CS3
|
1207457-11-1 |
CS3 is a potent, selective cIAP1 and cIAP2 inhibitor with IC50 of 16 nM and 85 nM respectively, shows no significant activity against XIAP (IC50>34 uM). |
| GY05340 |
PS1
|
1207994-72-6 |
PS1 is a potent inhibitor of IAP family with IC50 of 36/96/33 nM for c-IAP1/c-IAP2/XIAP respectively. |
| GY05319 |
T-3256336
|
1266227-69-3 |
A potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively; dose dependently antagonizes XIAP and promotes the activities of caspase-3 with EC50 of 1.3 uM in cell-free assays, induces the rapid proteasomal degradation of cIAP-1 and activates TNF-α-dependent extrinsic apoptosis signaling in cultured cells; induces cIAP-1 degradation, TNF-α production and caspase activation in cancer xenograft models. |
| GY05293 |
AT-IAP
|
1403898-55-4 |
A potent, orally bioavailable, dual XIAP/cIAP1 inhibitor with EC50 of 5.1/0.32 nM, respectively; exhibits MDA-MB-231 cell proliferation inhibition with IC50 of 4.4 nM; decreases basal and TNF-α-induced cIAP-1 expression in CaP cells, switches TNF-α signaling from pro-survival to pro-apoptotic and increases radiation sensitivity of CaP cells in co-culture with THP-1 cells; shows in vivo efficacy in Balb/c scid mice bearing MDA-MB-231 xenografts. |
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