BV6

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子二价 IAP 拮抗剂，可与 c-IAP1 和 XIAP BIR2-BIR3 结构域结合。

A small molecule, bivalent IAP antagonist that binds to the c-IAP1 and XIAP BIR2-BIR3 domains with Kd of 0.46 and 0.029 nM, respectively; results in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs; also induces induce TNFα-dependent cell death, exhibits single-agent cell killing activity in EVSA-T cell line (IC50=14 nM).

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.

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 mm2/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.

BV 6 | BV-6

Apoptosis

IAP

cIAP|XIAP

Cancer

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1001600-56-1

1205.573

C70H96N10O8

>98% (HPLC)

DMSO: ≥ 58 mg/mL

O=C([C@H]1N(C([C@H](C2CCCCC2)NC([C@@H](NC)C)=O)=O)CCC1)N[C@@H](C(C3=CC=CC=C3)C4=CC=CC=C4)C(NCCCCCCNC([C@@H](NC([C@H]5N(C([C@H](C6CCCCC6)NC([C@@H](NC)C)=O)=O)CCC5)=O)C(C7=CC=CC=C7)C8=CC=CC=C8)=O)=O

L-Phenylalaninamide, 4,4'-(1,6-hexanediyl)bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolyl-β-phenyl-

(-20℃)

With Ice Pack

≥ 2 years