IAP
特异性亚型抑制剂
IAP产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1130 |
YM155 (Sepantronium Bromide)YM155 (Sepantronium Bromide)是一种有效的survivin抑制药,通过抑制Survivin启动子活性而发挥作用,在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM;对SV40启动子活性抑制作用不显著,能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivin 和 XIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。 |
![]() ![]() MM cell lines UM9 (left panel) or U266 (right panel) were cultured in presence or absence of accessory cells prior to incubation with CTLs alone, YM155 alone or the combination. Survival of UM9 and U266 MM cells was assessed by CS-BLI. Results show % lysis of MM cells after 24 hour incubation and are depicted for three doses. |
|
S7597 |
BV-6BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。 |
![]() ![]() 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. |
|
S2271 |
Berberine chloride (NSC 646666)Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1,Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
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S5967 |
Berberine chloride hydrateBerberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8,poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。 |
||
S5600 |
Flavokawain AFlavokawain 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 |
AZD5582AZD5582,一种新型的小分子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。AZD5582 可诱导凋亡。 |
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S9634 |
Phenoxodiol (Haginin E)Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物,可激活 caspase 系统,抑制 XIAP (X-linked inhibitor of apoptosis),并破坏 FLICE inhibitory protein (FLIP) 的表达,从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。 |
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S7025 |
EmbelinEmbelin (Embelic Acid, NSC 91874),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。 |
![]() ![]() (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.
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S7009 |
LCL161LCL-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)。 |
![]() ![]() 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.
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S7015 |
Birinapant (TL32711)Birinapant (TL32711)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。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。 |
![]() ![]() 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-0152GDC-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。 |
![]() ![]() 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 |
Xevinapant (AT406)Xevinapant (AT406, ARRY-334543, Debio1143, SM-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。 |
![]() ![]() G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting. |
|
S7089 |
SM-164SM-164 是一种有效的、非肽类、细胞可渗透的 XIAP 的拮抗剂,靶向BIR2和BIR3结构域,其IC50值为1.39 nM。SM-164 可诱导凋亡和肿瘤消退。 |
||
S8681 |
Tolinapant (ASTX660)Tolinapant (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 |
---|---|---|---|
S1130 |
YM155 (Sepantronium Bromide)YM155 (Sepantronium Bromide)是一种有效的survivin抑制药,通过抑制Survivin启动子活性而发挥作用,在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM;对SV40启动子活性抑制作用不显著,能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivin 和 XIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。 |
![]() ![]() MM cell lines UM9 (left panel) or U266 (right panel) were cultured in presence or absence of accessory cells prior to incubation with CTLs alone, YM155 alone or the combination. Survival of UM9 and U266 MM cells was assessed by CS-BLI. Results show % lysis of MM cells after 24 hour incubation and are depicted for three doses. |
|
S7597 |
BV-6BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。 |
![]() ![]() 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. |
|
S2271 |
Berberine chloride (NSC 646666)Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8,分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1,Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
||
S5967 |
Berberine chloride hydrateBerberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8,poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。 |
||
S5600 |
Flavokawain AFlavokawain 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 |
AZD5582AZD5582,一种新型的小分子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。AZD5582 可诱导凋亡。 |
||
S9634 |
Phenoxodiol (Haginin E)Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物,可激活 caspase 系统,抑制 XIAP (X-linked inhibitor of apoptosis),并破坏 FLICE inhibitory protein (FLIP) 的表达,从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。 |
||
S7025 |
EmbelinEmbelin (Embelic Acid, NSC 91874),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。 |
![]() ![]() (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 |
LCL161LCL-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)。 |
![]() ![]() 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 (TL32711)Birinapant (TL32711)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。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。 |
![]() ![]() 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-0152GDC-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。 |
![]() ![]() 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 |
Xevinapant (AT406)Xevinapant (AT406, ARRY-334543, Debio1143, SM-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。 |
![]() ![]() G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting. |
|
S7089 |
SM-164SM-164 是一种有效的、非肽类、细胞可渗透的 XIAP 的拮抗剂,靶向BIR2和BIR3结构域,其IC50值为1.39 nM。SM-164 可诱导凋亡和肿瘤消退。 |
||
S8681 |
Tolinapant (ASTX660)Tolinapant (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。 |