PF-670462 2HCl
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货号：A124173
同义名：
PF-670462;PF-670462 dihydrochloride
PF-670462 is a potent and selective inhibitor of CK1ε with IC50 of 7.7 ± 2.2 nM.
PF-670462 2HCl 化学结构
PF-670462 2HCl 3D分子结构
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PF-670462 2HCl 纯度/质量文件 产品仅供科研
货号：A124173
标准纯度：
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产品说明书
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PF-670462 2HCl 质控信息
PF-670462 2HCl
++++
CK1ε, IC50: 90 nM
CK1δ, IC50: 13 nM
99%+
D4476
++
CK1 from Schizosaccharomyces pombe, IC50: 200 nM
CK1δ, IC50: 300 nM
98%
SR-3029
+++
CK1ε, IC50: 260 nM
CK1δ, IC50: 44 nM
99%+
IWP-2
+++
Wnt
98%
LY364947
++
98%
TA-01
++++
CK1ε, IC50: 6.4 nM
CK1δ, IC50: 6.8 nM
p38 MAPK
99%+
IC261
+
98%
PF-4800567
+++
casein kinase 1 epsilon, IC50: 32 nM
casein kinase 1 delta, IC50: 711 nM
99%+
CK1-IN-1
++++
CK1ε, IC50: 16 nM
CK1δ, IC50: 15 nM
98%
Longdaysin
+
CKIα, IC50: 5.6 μM
CKIδ, IC50: 8.8 μM
99%+
Silmitasertib
++++
99%+
Ellagic acid (hydrate)
+++
PKA
95+%
DMAT
+++
98%
Hematein
++
98+%
Silmitasertib sodium salt
++++
CK2α', IC50: 1 nM
CK2α, IC50: 1 nM
99%+
LY294002
+++
99%+
A-3 HCl
+
++
MLCK,PKA,PKC
98+%
TBB
+
++
98%
TTP 22
++
98%+
DRB
✔
99%+
BioE-1115
+
99%+
(E/Z)-GO289
++++
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
PF-670462 2HCl 生物活性
靶点
CK1
CK1ε, IC50:90 nM
CK1δ, IC50:13 nM
描述
CK1 kinases regulate diverse processes including Wnt signaling, membrane trafficking, the actin cytoskeleton, the DNA damage response, and circadian rhythms. Importantly, aberrant CK1δ and CK1ε activity is implicated in human pathologies, including neurodegenerative diseases, sleep disorders and cancer. PF-670462 is an effective and selective CK1ε and CK1δ inhibitor with IC50 s of 90 nM and 13 nM, respectively[3] E -cadherin expression, reaching a maximum effect at 3-10 μM PF670462. PF670462 (30 mg/kg/day, i.p.) attenuated bleomycin-induced accumulation of hydroxyproline and the number of infiltrating immune cells measured in the BAL fluid. In a separate study in female mice, aerosolised PF670462 (0.3-3.0 mg/ml, 15 min/once daily) corresponding to estimated deposited doses of ∼1-10 μg/day from day 8-20, also reduced hydroxyproline content, BALF cell influx, and fibrogenic gene expression at day 21[4]
PF-670462 2HCl 动物研究
Dose
Rat: 10 mg/kg, 30 mg/kg[3] [2]
Administration
s.c.
PF-670462 2HCl 参考文献
[1] Walton KM, Fisher K, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9.
[2] Badura L, Swanson T, et al. An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions. J Pharmacol Exp Ther. 2007 Aug;322(2):730-8.
[3] Bibian M, Rahaim RJ, Choi JY, Noguchi Y, Schürer S, Chen W, Nakanishi S, Licht K, Rosenberg LH, Li L, Feng Y, Cameron MD, Duckett DR, Cleveland JL, Roush WR. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. doi: 10.1016/j.bmcl.2013.05.075. Epub 2013 May 31. PMID: 23787102; PMCID: PMC3783656.
[4] Keenan CR, Langenbach SY, Jativa F, Harris T, Li M, Chen Q, Xia Y, Gao B, Schuliga MJ, Jaffar J, Prodanovic D, Tu Y, Berhan A, Lee PVS, Westall GP, Stewart AG. Casein Kinase 1δ/ε Inhibitor, PF670462 Attenuates the Fibrogenic Effects of Transforming Growth Factor-β in Pulmonary Fibrosis. Front Pharmacol. 2018 Jul 10;9:738. doi: 10.3389/fphar.2018.00738. PMID: 30042678; PMCID: PMC6048361.
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PF-670462 2HCl 实验方案
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摩尔计算器
总药量计算器
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存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.44mL
0.49mL
0.24mL
12.19mL
2.44mL
1.22mL
24.37mL
4.87mL
2.44mL
PF-670462 2HCl 技术信息
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