Bisindolylmaleimide XI hydrochloride

更新时间：2024-01-06 17:41:17

Bisindolylmaleimide XI hydrochloride结构式	常用名	Bisindolylmaleimide XI hydrochloride	英文名	Bisindolylmaleimide XI hydrochloride
	CAS号	145333-02-4	分子量	489.01
	密度	N/A	沸点	N/A
	分子式	C₂₈H₂₉ClN₄O₂	熔点	N/A
	MSDS	美版	闪点	N/A

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 ]。

中文名	二吲哚基马来酰亚胺XI盐酸盐
英文名	3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione,hydrochloride
英文别名	更多

描述	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 ]。
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.

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

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

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 ...

3-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl}-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride

3-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl}-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride (1:1)

1H-Pyrrole-2,5-dione, 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-, hydrochloride (1:1)