Birinapant

Birinapant 是一种二价 Smac 类似物，为XIAP 和 cIAP1的有效拮抗剂，Kd 值分别为 45 nM 和 < 1 nM。

MCE (MedChemExpress) 是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。MCE 的产品范围覆盖各种抑制剂、激动剂和化合物库。

Birinapant 是一种二价 Smac 类似物，为XIAP 和 cIAP1的有效拮抗剂，K_d 值分别为 45 nM 和 < 1 nM。
Birinapant产品描述：Birinapant a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with K_d values of 45 nM and < 1 nM, respectively.
In Vitro: Birinapant causes significant degradation of cIAP1 and 2. Birinapant + TRAIL-treated cells show increased levels of active caspase-8 and caspase-3, as well as PARP cleavage, over single agents within 4 h of treatment, indicative of apoptosis-mediated cell death. Birinapan significantly decreases the viability of SUM190 cells in a dose-dependent manner. Birinapant treatment in the XIAP knockdown cell line (SUM190 shXIAP) causes an overall reduction in viability at lower doses (30-300 nM)^[1]. Birinapant causes apoptosis in the sensitive cells. Birinapant in conbination with TNF-α, causes PARP cleavage in 451Lu and WM1366 cell lines^[2]. Birinapant induces time-course of caspase-3 activation in HCT116 human colon carcinoma and MDA-MB-231 human breast adenocarcinoma cells^[3].
In Vivo: Birinapant can inhibit tumor growth in melanoma xenotransplantation models. Staining for activated caspase-3 in biopsies of the same tumors show a modest increase in apoptotic cells in the birinapant treated animals^[2]. Birinapant (15 mg/kg, i.p.) induces apoptosis in HCT116 tumor-bearing mouse^[3].


公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和区总代理，营销网点遍及20多个地区。MCE经过多年努力已成为生物活性小分子领域的供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被近万名客户广泛使用并发表大量文章、；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供试用装； 已为多个知名企业、院校构建各种定制型化合物库。

Purity:98%
MWt:806.9409
Formula:C42H56F2N8O6
SMILES:FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2
Pathway:Apoptosis;
Mechanisms:IAP;
Research Area:Cancer




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