IAP

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抑制剂选择性比较

特异性亚型抑制剂

IAP产品

所有产品 IAP抑制剂(5) IAP拮抗剂(4)

目录号	产品描述	文献引用	实验数据
S7597	BV-6 BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。	Cell Death Differ, 2020, 26 Cancer Lett, 2020, 1;472:29-39 Cell Death Dis, 2020, 4;11(5):305	IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. P≤0.05, *P≤0.01.
S5600	Flavokawain A Flavokawain A 是一种从 kava 提取的凋亡诱导剂和抗癌剂。 Flavokawain A 可以下调抗凋亡蛋白，例如 XIAP、 survivin 和 Bcl-xL，从而改变凋亡与抗凋亡分子之间的平衡、诱导肿瘤细胞死亡。
S7362	AZD5582 AZD5582，一种新型的小分子IAP抑制剂，与cIAP1, cIAP2和XIAP的BIR3区域有效结合，IC50分别为15, 21, 15 nM。	Life Sci Alliance, 2020, 28;3(6) pii: e202000735 EMBO J, 2019, 15;38(10):e101638 Cell Chem Biol, 2019, 26(3):331-339
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。	Cell Host Microbe, 2018, 24(5):689-702 Am J Pathol, 2018, 188(2):404-416 Antiviral Res, 2018, 158:13-24	(d) Representative plots of apoptosis in Jurkat cells treated with vehicle only, BIO, CN585, Embelin (Emb), BIO plus CN585 or BIO plus CN585 plus Emb.
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)。	Cell Death Dis, 2020, 20;11(4):255 Apoptosis, 2020, 21 PLoS One, 2020, 15(1):e0228015	Parental or rVCR RD cells were either left untreated (UT) or exposed to 40 μM of LCL161 in the absence or presence of PSC-833 (10 μM) for 48 h before analysis of DNA fragmentation using PI staining and flow cytometry (data shown are mean + SD, n = 3). , p < 0.05, , p < 0.01, **, p < 0.001.
S7015	Birinapant Birinapant是一种SMAC模拟拮抗剂，对cIAP1最有效，无细胞试验中K_d为<1 nM，对XIAP作用较弱。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。	Cell Rep, 2020, 30(4):1260-1270 Cell Rep, 2020, 21;31(3):107547 Cell Death Differ, 2020, 26	Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.
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K_i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。	Apoptosis, 2020, 21 Theranostics, 2019, 9(9):2424-2438 Cell Chem Biol, 2019, 26(3):331-339	Inhibitor of Apoptosis Proteins (IAPs) were involved in MCP-1/IL-6 production under high dose TNF-α stimulation. A. hUC-MSCs (2x104 in 96-well plates) were pretreated for 2h with the IAP inhibitor GDC-0152 at increasing concentrations (0-1000 nM), then stimulated with TNF-α (20 ng/ml, 1.2 nM). After a further 24h, trypan blue was used to exclude cell toxicity. SN was collected and IL-6 and MCP-1 concentrations were measured by ELISA. B. hUC-MSCs(5×105 in T25 bottle) were pretreated with GDC-0152(1000nM) for 2 h, then stimulated with TNF-α (20 ng/ml, 1.2 nM). 24 hours later, protein from nucleus and cytoplasma were extracted separately and the amount of NF-kB were detected by Western blot. Data are as mean±SEM of triplicate measurements; p<0.05, p<0.01, **p<0.001 when compared to untreated cells. These experiments were repeated 3 times with the same results, using clone 69 and another TNF-α sensitive clone (clone 120003).
S2754	AT406 (SM-406) 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，K_i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。	Nature, 2020, 577(7788):109-114 Cell Death Dis, 2020, 22;11(5):391 Apoptosis, 2020, 21	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S8681^New	ASTX660 ASTX660 是一种有效的 cIAP1/2 和 XIAP 的非拟肽拮抗剂，可抑制SMAC衍生肽分别与XIAP的BIR3域（BIR3-XIAP）和cIAP1的BIR3域（BIR3-cIAP1）之间的相互作用，其IC50值分别小于40 nM和12 nM。

目录号	产品描述	文献引用	实验数据
S7597	BV-6 BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。	Cell Death Differ,2020, 26 Cancer Lett,2020, 1;472:29-39 Cell Death Dis,2020, 4;11(5):305	IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. P≤0.05, *P≤0.01.
S5600	Flavokawain A Flavokawain A 是一种从 kava 提取的凋亡诱导剂和抗癌剂。 Flavokawain A 可以下调抗凋亡蛋白，例如 XIAP、 survivin 和 Bcl-xL，从而改变凋亡与抗凋亡分子之间的平衡、诱导肿瘤细胞死亡。
S7362	AZD5582 AZD5582，一种新型的小分子IAP抑制剂，与cIAP1, cIAP2和XIAP的BIR3区域有效结合，IC50分别为15, 21, 15 nM。	Life Sci Alliance,2020, 28;3(6) pii: e202000735 EMBO J,2019, 15;38(10):e101638 Cell Chem Biol,2019, 26(3):331-339
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。	Cell Host Microbe,2018, 24(5):689-702 Am J Pathol,2018, 188(2):404-416 Antiviral Res,2018, 158:13-24	(d) Representative plots of apoptosis in Jurkat cells treated with vehicle only, BIO, CN585, Embelin (Emb), BIO plus CN585 or BIO plus CN585 plus Emb.
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)。	Cell Death Dis,2020, 20;11(4):255 Apoptosis,2020, 21 PLoS One,2020, 15(1):e0228015	Parental or rVCR RD cells were either left untreated (UT) or exposed to 40 μM of LCL161 in the absence or presence of PSC-833 (10 μM) for 48 h before analysis of DNA fragmentation using PI staining and flow cytometry (data shown are mean + SD, n = 3). , p < 0.05, , p < 0.01, **, p < 0.001.

目录号	产品描述	文献引用	实验数据
S7015	Birinapant Birinapant是一种SMAC模拟拮抗剂，对cIAP1最有效，无细胞试验中K_d为<1 nM，对XIAP作用较弱。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。	Cell Rep, 2020, 30(4):1260-1270 Cell Rep, 2020, 21;31(3):107547 Cell Death Differ, 2020, 26	Western blot analysis of XIAP and cIAP1 expression and PARP cleavage in H460, A549 and 34LU cells pre-treated with vorinostat or entinostat for 6h followed by the SMAC mimetic birinapant for 24h.
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K_i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。	Apoptosis, 2020, 21 Theranostics, 2019, 9(9):2424-2438 Cell Chem Biol, 2019, 26(3):331-339	Inhibitor of Apoptosis Proteins (IAPs) were involved in MCP-1/IL-6 production under high dose TNF-α stimulation. A. hUC-MSCs (2x104 in 96-well plates) were pretreated for 2h with the IAP inhibitor GDC-0152 at increasing concentrations (0-1000 nM), then stimulated with TNF-α (20 ng/ml, 1.2 nM). After a further 24h, trypan blue was used to exclude cell toxicity. SN was collected and IL-6 and MCP-1 concentrations were measured by ELISA. B. hUC-MSCs(5×105 in T25 bottle) were pretreated with GDC-0152(1000nM) for 2 h, then stimulated with TNF-α (20 ng/ml, 1.2 nM). 24 hours later, protein from nucleus and cytoplasma were extracted separately and the amount of NF-kB were detected by Western blot. Data are as mean±SEM of triplicate measurements; p<0.05, p<0.01, **p<0.001 when compared to untreated cells. These experiments were repeated 3 times with the same results, using clone 69 and another TNF-α sensitive clone (clone 120003).
S2754	AT406 (SM-406) 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，K_i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。	Nature, 2020, 577(7788):109-114 Cell Death Dis, 2020, 22;11(5):391 Apoptosis, 2020, 21	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S8681^New	ASTX660 ASTX660 是一种有效的 cIAP1/2 和 XIAP 的非拟肽拮抗剂，可抑制SMAC衍生肽分别与XIAP的BIR3域（BIR3-XIAP）和cIAP1的BIR3域（BIR3-cIAP1）之间的相互作用，其IC50值分别小于40 nM和12 nM。