IAP

Inhibitory Selectivity

Catalog No.	Inhibitor Name	cIAP	XIAP	Other
A12738	Birinapant	****	**
A14135	GDC-0152	***	***	MLXBIR3SG
A13055	Embelin		*	5-LO,mPGES-1
A14231	BV-6
A11928	LCL161
A15800	SM-164	****	****
A11163	AT406 (SM-406)	****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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AT-406 (SM-406, ARRY-334543)

Catalog No. A11163
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IAP 抑制剂

AT-406 (SM-406,ARRY-334543)是IAP家族蛋白质的口服生物利用抑制剂，具有潜在的凋亡诱导和抗肿瘤活性。AT-406选择性抑制IAP蛋白的生物学活性，包括X染色体连锁IAP（XIAP），细胞IAP 1（c-IAP1）和2（c-IAP2）和黑色素瘤凋亡抑制蛋白（ML-IAP）。了解更多

Product Citations (2)

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- Yoshikawa M, .et al. Discovery of 7-Oxo-2,4,5,7-tetrahydro-6 H-pyrazolo[3,4- c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure-Kinetic Relationships, J Med Chem, 2018, Mar 22;61(6):2384-2409 PMID: 29485864
- Tsuyoshi Ishii, .et al. CETSA quantitatively verifies in vivo target engagement of novel RIPK1 inhibitors in various biospecimens, Sci Rep, 2017, 7: 13000 PMID: 29026104
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LCL-161

Catalog No. A11928
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拮抗剂of IAPs抑制剂

LCL161是口服生物可利用的第二个线粒体衍生的半胱天冬酶（SMAC）类似物激活剂，也是IAP（细胞凋亡抑制蛋白）家族蛋白的抑制剂，具有潜在的抗肿瘤活性，抑制 HEK293 细胞中 XIAP 和 MDA-MB-231细胞中 cIAP1 的 IC50分别为 35 和 0.4 nM。了解更多

Product Citations (7)

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- Han-Hee Park, .et al. RIPK3 activation induces TRIM28 derepression in cancer cells and enhances the anti-tumor microenvironment, Mol Cancer, 2021, Aug 21;20(1):107 PMID: 34419074
- Se-Yeon Park, .et al. Reduction in MLKL-mediated endosomal trafficking enhances the TRAIL-DR4/5 signal to increase cancer cell death, Cell Death & Disease, 2020, 11:744 PMID: 32917855
- J Chen, .et al. Interferon-γ induces the cell surface exposure of phosphatidylserine by activating MLKL in the absence of caspase-8 activity, JBC, 2019, June PMID: 31217278
- Choi SW, .et al. PELI1 Selectively Targets Kinase-Active RIP3 for Ubiquitylation-Dependent Proteasomal Degradation, Mol Cell, 2018, Jun 7;70(5):920-935.e7 PMID: 29883609
- Han-Hee Park, .et al. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis, Exp Mol Med, 2018, Sep; 50(9): 125 PMID: 30237400
- Gi-Bang Koo, .et al. Methylation-dependent loss of RIP3 expression in cancer represses programmed necrosis in response to chemotherapeutics, Cell Res, 2015, Jun; 25(6): 707-725 PMID: 25952668
- Kim SK, .et al. Upregulated RIP3 Expression Potentiates MLKL Phosphorylation-Mediated Programmed Necrosis in Toxic Epidermal Necrolysis, J Invest Dermatol, 2015, Aug;135(8):2021-2030 PMID: 25748555
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BV-6

Catalog No. A14231
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dual cIAP and XIAP 抑制剂

BV-6是一种SMAC模拟，双重cIAP和XIAP抑制剂。了解更多

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- Aneri Shah, .et al. YB-1 Mediates TNF-Induced Pro-Survival Signaling by Regulating NF-κB Activation, Cancers (Basel), 2020, Aug 5;12(8):E2188 PMID: 32764479
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SM-164

Catalog No. A15800
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cIAP-2 拮抗剂

SM-164是一种有效的细胞渗透性二价Smac模拟物，它与KiAP为0.56 nM的XIAP蛋白结合，并分别与Ki值为0.31和1.1 nM的cIAP-1和cIAP-2蛋白结合。了解更多

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- Hanna Yuk, .et al. Necrostatin-1 Prevents Ferroptosis in a RIPK1- and IDO-Independent Manner in Hepatocellular Carcinoma, Antioxidants (Basel), 2021, Aug 25;10(9):1347 PMID: 34572979
- Caroline Moerke, .et al. The anticonvulsive Phenhydan® suppresses extrinsic cell death, Cell Death Differ, 2018, Nov 15 PMID: 30442947
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Birinapant (TL32711)

Catalog No. A12738
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XIAP/cIAP1 拮抗剂

Birinapant (TL32711)是第二个线粒体衍生的胱天蛋白酶（SMAC）激活剂和IAP（凋亡蛋白抑制剂）家族蛋白抑制剂的合成小分子和肽类似物，对cIAP1最有效，无细胞试验中Kd为<1 nM，具有潜在的抗肿瘤活性。了解更多

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GDC-0152

Catalog No. A14135
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IAP 拮抗剂

GDC-0152是caspases（Smac）的第二个线粒体激活物，具有潜在的抗肿瘤活性。了解更多

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Embelin

Catalog No. A13055
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XIAP 抑制剂

Embelin是一种细胞可渗透的苯醌化合物，具有抗肿瘤特性。了解更多

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Apoptosis Inhibitor (M50054)

Catalog No. A13058
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Apoptosis 抑制剂

Apoptosis Inhibitor (M50054)是细胞可渗透的凋亡诱导抑制剂。了解更多

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