XIAP 选择性抑制剂 | 拮抗剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S7089 SM-164

SM-164 is a cell-permeable Smac mimetic compound that binds to XIAP protein containing both the BIR2 and BIR3 domains with IC50 of 1.39 nM and functions as an extremely potent antagonist of XIAP.

Selective XIAP, IC50: 1.39 nM
S7025 Embelin

Embelin,从矮地茶中分离的一种醌类化合物,是一种细胞凋亡的X染色体抑止剂(XIAP)的抑制剂,无细胞试验中IC50为4.1 μM。

Selective XIAP, IC50: 4.1 μM
S9634 Phenoxodiol (Haginin E)

Phenoxodiol inhibits XIAP (an apoptosis inhibitor) and DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol activates the mitochondrial caspase system and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol is a synthetic analog of Genestein.

S5600 Flavokawain A

Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.

S7362 AZD5582

AZD5582,一种新型的小分子IAP抑制剂,与cIAP1, cIAP2XIAP的BIR3区域有效结合,IC50分别为15, 21, 15 nM。

Pan XIAP, IC50: 15 nM
S7010 GDC-0152

GDC-0152是一种有效的XIAP-BIR3,ML-IAP-BIR3,cIAP1-BIR3和cIAP2-BIR3拮抗剂,无细胞试验中Ki分别为28 nM,14 nM,17 nM和43 nM,对cIAP1-BIR2和cIAP2-BIR2具较低亲和力。Phase 1。

Pan XIAP-BIR2, Ki: 112 nM; XIAP-BIR3, Ki: 28 nM
S8681 Tolinapant (ASTX660)

Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.

Pan XIAP, IC50: 40 nM
S7015 Birinapant (TL32711)

Birinapant是一种SMAC模拟拮抗剂,对cIAP1最有效,无细胞试验中Kd为<1 nM,对XIAP作用较弱。Phase 2。

Pan XIAP, Kd: 45 nM
S2754 Xevinapant (AT406)

AT-406是一种有效的,拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂,与XIAP-BIR3, cIAP1-BIR3和cIAP2-BIR3结合,Ki为66.4 nM, 1.9 nM和5.1 nM,比作用于Smac AVPI肽亲和力高50到100倍。Phase 1。

Pan XIAP-BIR3, Ki: 66.4 nM
S7009 LCL161

LCL-161, 一种second mitochondrial activator of caspase (SMAC, 线粒体促凋亡蛋白)模拟物, 能有效地结合并抑制多种IAPs(i.e. XIAP, c-IAP)。

S7597 BV-6