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Submit ReviewG 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.
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 |
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.
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 |
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.
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
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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