NSC-23766 Rac1 GTPase抑制剂 733767-34-5

保存条件 ：零下20度

保质期 ：3年

英文名 ：NSC-23766

库存 ：大量

供应商 ：上海惠诚生物科技有限公司

CAS号 ：733767-34-5

规格 ：5 mg/25 mg

NSC-23766 (733767-34-5) is a selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) Trio and Tiam1 (IC₅₀ ca. 50 μM) with no effect on the closely related Cdc42 or RhoA. In cells, it blocks serum or PDGF-induced Rac-1 activation and lamellipodia formation. NSC-23766 suppressed the growth of wild-type NIH 3T3 cells but was inactive in cells expressing the constitutively active Rac1 mutant, L61Rac1.¹ It is a useful tool to probe the involvement of Rac1 in cell signalling.² Off target effect: antagonist at muscarinic acetylcholine receptors.³ Cell permeable.
NSC-23766(733767-34-5)是Rac1-GEF相互作用的选择性抑制剂。 抑制Rac1特异性鸟嘌呤核苷酸交换因子(GEFs) Trio和Tiam1 (IC50约50 μM)激活，对密切相关的Cdc42或RhoA无影响。 在细胞中，它可以阻断血清或pdgf诱导的Rac-1激活和板瓣的形成。 NSC-23766抑制了野生型NIH 3T3细胞的生长，但在表达组成性活性Rac1突变体L61Rac1.1的细胞中不活跃。这是研究Rac1参与细胞信号传导的有用工具 脱靶效应:毒蕈碱乙酰胆碱受体拮抗剂 细胞的渗透。

References/Citations:

1. Gao et al. (2004), Rational design and characterization of a Rac GTPase-specific small molecule inhibitor; Proc. Natl. Acad. Sci. USA, 101 7618
2. Shankar et al. (2013), Raft endocytosis of AMF regulates mitochondrial dynamics through Rac1 signaling and the Gp78 ubiquitin ligase; J. Cell Sci., 126 3295
3. Levay et al. (2013), NSC23766, a widely used inhibitor of Rac1 activation, additionally acts as a competitive antagonist at muscarinic acetylcholine receptors; J. Pharmacol. Exp. Ther., 347 69

CAS:
733767-34-5
Catalog Number:
10-2731
Activity:
Rac1 GTPase inhibitor
Chemical Names:
N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Molecular Weight:
530.98
Molecular Formula:
C₂₄H₃₅N₇·3HCl
Solubility:
Soluble in DMSO (50 mg/ml); Water (50 mg/ml)
Physical Properties:
White solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
Room temperature
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT
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