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PF-670462 dihydrochloride | MedChemExpress (MCE)

英文名称:PF-670462 dihydrochloride
品牌 厂商性质 产地 货期 价格
MedChemExpress (MCE) 生产商 美国 现货 1351

性能特点

PF-670462 dihydrochloride 是一种有效的,选择性的 casein kinase (CKIε/CKIδ) 抑制剂,IC50 值分别为 7.7 nM 和 14 nM。

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产品参数
规格 CAS号 价格 操作
10 mM * 1 mL 950912-80-8 ¥1,351.00 询底价
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PF-670462 dihydrochloride

CAS No. : 950912-80-8

MCE 国际站:PF-670462 dihydrochloride

产品活性:PF-670462 dihydrochloride 是一种有效的,选择性的 casein kinase (CKIε/CKIδ) 抑制剂,IC50 值分别为 7.7 nM 和 14 nM。

研究领域:Cell Cycle/DNA Damage  |  Stem Cell/Wnt

作用靶点:Casein Kinase

In Vitro: PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC50s of 7.7 nM and 14 nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC50s of 150 nM and 190 nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC50 of 290 ± 39 nM in CKIε-transfected COS7 cells. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC50 of ∼17 nM. PF-670462 (1 μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100 nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling.

In Vivo: PF-670462 (50 mg/kg, s.c.) produces robust phase delays, and the activity remains persistent, with no discernible correction in the absence of exogenous zeitgebers in rats. PF-670462 (25, 50, and 100 mg/kg, s.c.) induces dose-dependent phase shift. PF-670462 (50 mg/kg; s.c.) significantly phase delays the rhythmic transcription of Bmal1, Per1, Per2 and Nr1d1 in both liver and pancreas by 4.5 ± 1.3 h and 4.5 ± 1.2 h, respectively, 1 day after administration. In the suprachiasmatic nucleus (SCN), the rhythm of Nr1d1 and Dbp mRNA expression is also delayed by 4.2 and 4 h, respectively.

相关产品:Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Serine/Threonine Kinase Inhibitor Library  |  Multi-Target Compound Library  |  LY294002  |  Silmitasertib  |  IWP-2  |  Emodin  |  Ellagic acid  |  D4476  |  Umbralisib  |  TBB  |  TMX-4116  |  Casein Kinase inhibitor A51  |  DMAT  |  PF-4800567  |  SR-3029  |  (E/Z)-GO289  |  FPFT-2216  |  SSTC3  |  IC261  |  TAK-715  |  SGC-CK2-1  |  CKI-7 free base  |  TTP 22  |  BioE-1115  |  CK1-IN-1  |  AMG-548 dihydrochloride  |  BTX161  |  PF-5006739  |  TA-01  |  CK2/ERK8-IN-1  |  Hematein

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