SML3237
G-5555
≥98% (HPLC)
别名:
8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one, 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
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About This Item
一般描述
G-5555 is a selective p21-activated kinase (PAK1) inhibitor. In addition to this it also selectively inhibits eight kinases such as PAK2, PAK3, KHS1, lymphocyte-specific protein tyrosine kinase (LcK), Mammalian Ste20-like kinase 3 (MST3), Mammalian Ste20-like kinase 4 (MST4), salt-inducible kinase 2(SIK2), and Yeast Sps1/Ste20-related Kinase 1 (YSK1). G-5555 exhibits high stability and low human ether-à-go-go related gene (hERG) activity than other PAK inhibitors including FRAX1036.
生化/生理作用
G-5555 is an ATP site-targeting inhibitor against salt-inducible kinases, MST3/4, p21-activated kinase 1/2, YANK1/3, MAP2K5, MAP4K5 (% inhibition at 100 nM = 98.6/93.5/99.8 (SIK1/2/3), 85/99.5 (MST3/4), 95.6/87 (PAK1/2), 94.7/96.5 (YANK1/3); 87/MAP2K5, 83/MAP4K5) with good selectivity over other kinases. G-5555 downregulates MEK pS298 in EBC1 cells in cultures (IC50 = 69 nM) and in H292 NSCLC tumors in mice in vivo (25 mg/kg p.o.) with good oral availability (mice F = 80%, monkeys F = 72%).
G-5555 is an ATP site-targeting inhibitor against salt-inducible kinases, MST3/4, p21-activated kinase 1/2, YANK1/3, MAP2K5, MAP4K5 (% inhibition at 100 nM = 98.6/93.5/99.8 (SIK1/2/3), 85/99.5 (MST3/4), 95.6/87 (PAK1/2), 94.7/96.5 (YANK1/3); 87/MAP2K5, 83/MAP4K5) with good selectivity over other kinases. G-5555 downregulates MEK pS298 in EBC1 cells in cultures (IC50 = 69 nM) and in H292 NSCLC tumors in mice in vivo (25 mg/kg p.o.) with good oral availability (mice F = 80%, monkeys F = 72%). PAK1 plays a crucial role in cancer progression, inhibiting this protein has the potential to reduce cancer development. Therefore, G-5555 may be a promising candidate for oncology research.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Chudi O Ndubaku et al.
ACS medicinal chemistry letters, 6(12), 1241-1246 (2015-12-30)
Signaling pathways intersecting with the p21-activated kinases (PAKs) play important roles in tumorigenesis and cancer progression. By recognizing that the limitations of FRAX1036 (1) were chiefly associated with the highly basic amine it contained, we devised a mitigation strategy to
Christina M Knippler et al.
Endocrine-related cancer, 26(8), 699-712 (2019-05-31)
The number of individuals who succumb to thyroid cancer has been increasing and those who are refractory to standard care have limited therapeutic options, highlighting the importance of developing new treatments for patients with aggressive forms of the disease. Mutational
Hai-Feng Qiao et al.
Journal of reproductive immunology, 140, 103129-103129 (2020-04-26)
The present study was meant for the discovery of the underlying functions of miR-485-5p in ovarian cancer concerning cisplatin resistance in vitro. RT-qPCR assessed the miR-485-5p expression in ovarian cancer cell lines, normal cells and cisplatin-resistant Cell line OVCA433-CR. After
Roberta Tesch et al.
Journal of medicinal chemistry, 64(12), 8142-8160 (2021-06-05)
Salt-inducible kinases (SIKs) are key metabolic regulators. The imbalance in SIK function is associated with the development of diverse cancers, including breast, gastric, and ovarian cancers. Chemical tools to clarify the roles of SIK in different diseases are, however, sparse
Hai-Feng Qiao et al.
Journal of reproductive immunology, 140, 103129-103129 (2020-04-26)
The present study was meant for the discovery of the underlying functions of miR-485-5p in ovarian cancer concerning cisplatin resistance in vitro. RT-qPCR assessed the miR-485-5p expression in ovarian cancer cell lines, normal cells and cisplatin-resistant Cell line OVCA433-CR. After
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