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抑制剂/激活剂

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凋亡与自噬

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Birinapant (TL32711)

Birinapant (TL32711) 比瑞那帕; 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。Birinapant可帮助诱导HIV-1感染的细胞凋亡。Phase 2。

货号：
TK0192
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1260251-31-7
生物活性	Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
分子式	C42H56F2N8O6
分子量	806.94
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 250 mg/mL (309.81 mM; Need ultrasonic) Ethanol : 25 mg/mL (30.98 mM; Need ultrasonic)
体内研究	Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models.
体外研究	Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner. Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis. Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation.
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纯度及产品资料	98%

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