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抑制剂/激活剂

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凋亡与自噬

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BV6

BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。

货号：
TK0171
规格：

1mg

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1001600-56-1
生物活性	BV6 is an antagonist of cIAP1 and XIAP, members of the inhibitors of apoptosis (IAP) family.
分子式	C70H96N10O8
分子量	1205.57
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : ≥ 58 mg/mL (48.11 mM)
体内研究	Murine cIAP-1, cIAP-2 and XIAP expressions are clearly observed in the cytoplasm of both epithelial and stromal cells of implants, whereas Survivin is mainly expressed in the nuclei BV6 treatment for 4 weeks attenuated the intensity of IAPs expression. The size of lesions range from ~2 to 7 mm in diameter. The monolayer epithelial cell lining of the cyst is shown. After immunohistochemical staining, cytokeratin and vimentin are positively stained, whereas calretinin is negative. After BV6 treatment for 4 weeks, the total number of lesions (4.6 versus 2.8/mouse), the average weight (78.1 versus 32.0 mg/mouse) and the surface area (44.5 versus 24.6 mm/mouse) of lesions are significantly less than in the controls. In the endometrial gland epithelia or stroma, the percentage of Ki67-positive cells decreases after BV6 treatment.
体外研究	HCC193 has an IC50 of 7.2 μM in MTS assays, while H460 cells are not reduced to 50% viability even with 30 μM BV6 treatment. Administration of 1 μM BV6 to HCC193 cells induces complete depletion of cIAP1 levels at 1 hour post-treatment, while a decrease in XIAP levels is not seen until 24 hours following addition of drug. Similarly, 5 μM BV6 fully depletes cIAP1 at 1 hour and begin to reduce XIAP at 24 hours in H460 cells. In parallel findings, cIAP1 levels are decreased in response to a small dose of 0.25 μM BV6 in both cell lines, whereas trace amounts of XIAP are still present at 5μM BV6. HCC193 cells demonstrates noticeable cleaved caspase-3 levels beginning 12 hours post-incubation with 1μM BV6, and cleaved caspase-3 levels continued to increase in a time-dependent manner over 48 hours. Treatment of HCC193 cells with 1 μM BV6 for 24 hours causes a significant survival curve shift in HCC193 cells relative to DMSO-treated cells, with a DER=1.38 (p<0.05). BV6 (2 and 5 µM) significantly represses BrdU incorporation in ectopic and eutopic (disease-free and myomas) ESCs. An ~30% decrease of BrdU incorporation is observed in both groups after treatment with 5 µM BV6.
文献	暂无相关参考文献
纯度及产品资料	98%

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