G 5555

Pricing Availability   Qty
说明: High affinity group I PAK inhibitor
化学名: 8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
纯度: ≥98% (HPLC)
说明书
引用文献 (1)
评论

生物活性 for G 5555

G 5555 is a high affinity group 1 PAK (pan-PAK1, 2 and 3) inhibitor (Ki = 3.7 nM; pMEK IC50 = 69 nM). Of 235 kinases tested, other than PAK1, eight (PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1) were inhibited >70%. Exhibits low hERG channel activity (<50% inhibition at 10 μM). Orally bioavailable.

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of G 5555 is reviewed on the chemical probes website.

技术数据 for G 5555

分子量 492.96
公式 C25H25ClN6O3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1648863-90-4
PubChem ID 91664373
InChI Key ZBCMHWUFWQFPLV-UHFFFAOYSA-N
Smiles CNC1=NC=C2C=C(C3=C(C=C(C4=CC=CC(C)=N4)C=C3)Cl)C(N(C2=N1)C[C@H]5OC[C@@H](CO5)N)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for G 5555

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
1eq. HCl 49.3 100
DMSO 9.86 20 温和加热

制备储备液 for G 5555

以下数据基于产品分子量 492.96。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.03 mL 10.14 mL 20.29 mL
5 mM 0.41 mL 2.03 mL 4.06 mL
10 mM 0.2 mL 1.01 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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参考文献 for G 5555

参考文献是支持产品生物活性的出版物。

Ndubaku et al (2015) Design of selective PAK1 inhibitor G-5555: improving properties by employing an unorthodox low-pK a polar moiety. ACS Med.Chem.Lett. 6 1241 PMID: 26713112


If you know of a relevant reference for G 5555, please let us know.

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关键词: G 5555, G 5555 supplier, G5555, Selective, high, affinity, group, 1, PAK, pan-PAK1, PAK2, PAK3, inhibitors, inhibits, orally, bioavailable, p21, activated, kinase, P21-activated, Kinases, 6051, Tocris Bioscience

1 篇 G 5555 的引用文献

引用文献是使用了 Tocris 产品的出版物。 G 5555 的部分引用包括:

Teresa L et al (2021) PAK1 Positively Regulates Oligodendrocyte Morphology and Myelination. J Neurosci 41 1864-1877 PMID: 33478987


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