YKL-05-099|1936529-65-5|-陌孚医药/Medlife

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YKL-05-099

目录号: PL11112 纯度: ≥99%

CAS No. :1936529-65-5

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中文名称	YKL-05-099
中文别名	YKL 05-099;化合物YKL-05-099;3-(2-氯-6-甲基苯基)-7-((2-甲氧基-4-(1-甲基哌啶-4-基)苯基)氨基)-1-(5-甲氧基吡啶-2-基)-3,4-二氢嘧啶并[4,5-D]嘧啶-2(1H)-酮
英文名称	YKL-05-099
英文别名	YKL-05-099;3-(2-Chloro-6-methylphenyl)-7-((2-methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-1-(5-methoxypyridin-2-yl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one;BDBM192716;BCP20631;SB18778;3-(2-Chloro-6-methylphenyl)-7-[2-methoxy-4-(1-methylpiperidin-4-yl)anilino]-1-(5-methoxypyridin-2-yl;s9646;3-(2-chloro-6-methylphenyl)-7-[2-methoxy-4-(1-methylpiperidin-4-yl)anilino]-1-(5-methoxypyridin-2-yl)-4H-pyrimido[4,5-d]pyrimidin-2-one;CID 121596782;Pyrimido[4,5-d]pyrimidin-2(1H)-one, 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-;YKL05099,YKL 05 099,inhibit,Salt-inducible Kinase (SIK),Inhibitor
Cas No.	1936529-65-5
分子式	C₃₂H₃₄ClN₇O₃
分子量	600.11
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	YKL-05-099 是一种盐诱导型激酶 (SIK) 抑制剂。YKL-05-099 作用于SIK1 和 SIK3，IC₅₀ 分别约为 10 和 30 nM。YKL-05-099 抑制 SIK2 的活性稍低，IC₅₀ 值为 40 nM。
生物活性	YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC 50 s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC 50 =40 nM).
性状	Solid
IC50 & Target[1][2]	IC50: 10 nM (SIK1), 30 nM (SIK3), 40 nM (SIK2)
体外研究(In Vitro)	YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM) and IL-10-enhancing activities (EC50=460 nM). YKL-05-099 binds to SIK1 and SIK3 with IC50s of 10 and 30 nM, respectively, in a competitive binding assay. Preincubating bone marrow-derived macrophages with YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259. YKL-05-099 suppresses production of the inflammatory cytokines TNFα, IL-6 and IL-12p40, and only modestly enhances IL-1β release in BMDCs stimulated with the yeast cell wall extract Zymosan A. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	YKL-05-099 is non-toxic at concentrations less than 10 μM and stable in mouse liver microsomes for more than 2 hours. YKL-05-099 is highly soluble (PBS solubility=428 μM) and present in an unbound state at appreciable levels in mouse plasma. YKL-05-099 dose dependently decreases phosphorylation of HDAC5 at the SIK-regulated site Ser259; reduced phosphorylation is observed at the lowest dose (5 mg/Kg) and is below the limit of detection by immunoblotting beginning at the 20 mg/Kg dose. YKL-05-099 dose-dependently reduces abundance of TNFα in serum beginning at 5 mg/Kg, and increases IL-10 levels at the 20 mg/Kg dose by more than 2-fold. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Sundberg TB, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 Aug 19;11(8):2105-11.

溶解度数据	In Vitro: DMSO : ≥ 75 mg/mL (124.98 mM)配制储备液

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