Bisindolylmaleimide XI hydrochloride

Bisindolylmaleimide XI hydrochloride用途

双吲哚酰马来酰亚胺席夫碱(RO 32-0432)是一种具有选择性、口服活性的PKC抑制剂,其对PKCα、PKCβI、PKCβII、PKCγ、PKCε分别为9 nm、28 nm、31 nm、37 nm和108 nm,分别为[1 ] [2 ]。

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Bisindolylmaleimide XI hydrochloride名称

[ CAS 号 ]:
145333-02-4

[ 中文名 ]:
二吲哚基马来酰亚胺XI盐酸盐

[ 英文名 ]:
Bisindolylmaleimide XI hydrochloride

[英文别名 ]:

Bisindolylmaleimide XI hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 炎症/免疫

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[ 靶点 ]

PKC-α:9 nM (IC50)

PKC-βI:28 nM (IC50)

PKC-βII:31 nM (IC50)

PKC-γ:37 nM (IC50)

PKC-ε:108 nM (IC50)

[体外研究]

双吲哚酰马来酰亚胺席夫碱(RO 32-0432)抑制佛波酯与植物血凝素或抗CD3刺激的外周人类T细胞IL-2分泌、IL-2受体表达和增殖,但不抑制IL-2诱导的细胞表达已被刺激表达IL-2受体的增殖。BidimoLyl马来酰亚胺席夫盐酸盐(2)抑制了流感肽抗原HA307～319-特异性人T细胞克隆(HA27)暴露于抗原脉冲自递呈细胞后的增殖。用双吲哚马来酰亚胺席夫碱(RO 32-0432；1μm)抑制PKC对视网膜祖细胞(RPC)凋亡细胞比例(-21%)的影响(3)。

[体内研究]

口服双吲哚马来酰亚胺席夫碱抑制随后的佛波酯诱导的大鼠水肿。由比索吲哚马来酰亚胺席夫盐酸盐(2)抑制了更多生理T细胞驱动的反应,如宿主对移植物反应和辅助性关节炎引起的继发性爪肿胀。

[参考文献]

[1]. S E Wilkinson, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2)(Pt 2):335-7.

[2]. A M Birchall, et al. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J Pharmacol Exp Ther. 1994 Feb;268(2):922-9.

[3]. Roman Kholodenko, et al. Anti-apoptotic effect of retinoic acid on retinal progenitor cells mediated by a protein kinase A-dependent mechanism. Cell Res. 2007 Feb;17(2):151-62.

Bisindolylmaleimide XI hydrochloride物理化学性质

[ 分子式 ]:
C₂₈H₂₉ClN₄O₂

[ 分子量 ]:
489.01

[ 精确质量 ]:
488.197906

[ PSA ]:
59.27000

[ LogP ]:
4.95500

[ 储存条件 ]:
2-8°C，惰性气体保护

Bisindolylmaleimide XI hydrochloride安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

Bisindolylmaleimide XI hydrochloride文献

Inhibition of PTH desensitization by inhibition of the G protein-coupled receptor kinase-5 enzyme with Ro 32-0432. Moore, J.B., et al.

FASEB J. 12 , A741, (1998)

Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.

Biochem. J. 294 , 335-337, (1993)

The protein kinase C (PKC) family of isoenzymes is believed to mediate a wide range of signal-transduction pathways in many different cell types. A series of bisindolylmaleimides have been evaluated a...

Cardiorespiratory responses to systemic administration of a protein kinase C inhibitor in conscious rats.

J. Appl. Physiol. 84 , 641-648, (1998)

Although protein kinase C (PKC) is an essential component of multiple neurally mediated events, its role in respiratory control remains undefined. The ventilatory effects of a systemically active PKC ...

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