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CLK1-IN-3

CAS No. 2922550-28-3

CLK1-IN-3( —— )

Catalog No. M36407 CAS No. 2922550-28-3

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CLK1-IN-3
  • Note
    Research use only, not for human use.
  • Brief Description
    Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A.
  • Description
    CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.
  • In Vitro
    Western Blot AnalysisCell Line:Hela cells, BNLCL.2 and HCT 116 cells Concentration:0.2, 1, 5, and 10 μM Incubation Time:24 h Result:Elevated the expression level of LC3II protein (a marker of autophagosomes) as well as the ratio of LC3II to LC3I (a sensitive index of autophagy) in a dose-dependent and time-dependent manner.
  • In Vivo
    Animal Model:Male C57BL/6 mice(8 weeks, injected acetaminophen (HY-66005) (500 mg/kg, ip))Dosage:10, 20, and 40 mg/kg Administration:IP, onceResult:Decreased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels significantly in dose-dependent.Animal Model:Male Balb/c mice (aged 8 weeks)Dosage:10 mg/kg Administration:IV, PO, IP, once (Pharmacokinetic Analysis) Result:Pharmacokinetic Parameters of CLK1-IN-3 in male Balb/C mice.
  • Synonyms
    ——
  • Pathway
    Autophagy
  • Target
    Autophagy
  • Recptor
    Autophagy | DYRK | CDK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2922550-28-3
  • Formula Weight
    430.48
  • Molecular Formula
    C24H23FN6O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (232.30 mM; Ultrasonic )
  • SMILES
    O=C(NC=1C=NC=2NC=C(C=3C=NC=C(F)C3)C2C1)C4=CC=C(C=C4)N5CCN(C)CC5
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Yang T, et al. Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI). Eur J Med Chem. 2023 Mar 15;250:115168.?
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