1. Cell Cycle/DNA Damage
  2. CDK

CLK1-IN-1 

Cat. No.: HY-103082 Purity: 99.03% ee.: 99.98%
Handling Instructions

CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.

For research use only. We do not sell to patients.

CLK1-IN-1 Chemical Structure

CLK1-IN-1 Chemical Structure

CAS No. : 2123491-32-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.

IC50 & Target

CLK1

2 nM (IC50)

In Vitro

CLK1 is the most potently inhibited kinase (IC50: 2 nM). In addition to CLK1, only two kinases have an IC50 value less than 100 nM, namely CLK2 (IC50: 31 nM) and CLK4 (IC50: 8 nM), DYRK1A is the strongest off-target. The ability of CLK1-IN-1 to induce autophagy in BNL CL.2 and SKOV-3 (human ovarian cancer cell line) cells is also examined. The effects of CLK1-IN-1 on yellow LC3 puncta also displays obvious dose dependency, and a dose of 10 μM shows the best performance. In addition, in CLK1-IN-1-treated cells, the number of red LC3 puncta (mRFP signals only35) increases compared with that of DMSO-treated cells, indicating the formation of autolysosomes. Importantly, CLK1-IN-1 stimulats the degradation of SQSTM1/p62 and increases the ratio of red LC3 puncta to yellow LC3 puncta, both of which indicate an induction of autophagic flux by CLK1-IN-1[1].

In Vivo

APAP exposure results in severe liver injury, and treatment with CLK1-IN-1 (ip, 30 mg/kg) imparts a significant hepatoprotective effect. The results show that treatment with CLK1-IN-1 decreases serum ALT and AST levels significantly such that both marker enzymes return to normal levels[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (122.12 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4425 mL 12.2124 mL 24.4248 mL
5 mM 0.4885 mL 2.4425 mL 4.8850 mL
10 mM 0.2442 mL 1.2212 mL 2.4425 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

BNL CL.2 (mouse embryonic liver cell line) is selected, and three concentrations (20 nM, 100 nM, and 10 μM) of CLK1-IN-1 are used[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Drug-induced liver injury (DILI) is a major public health concern and accounts for more than 50% of acute liver failure cases. APAP is a widely used antipyretic analgesic drug. Herein, the APAP-induced hepatotoxicity mouse model is used to examine the therapeutic effect of CLK1-IN-1 in vivo. Male C57BL/6 mice are given either saline (n=3, ip) or APAP (500 mg/kg) (n=15, ip). To examine the hepatoprotective effect, mice are injected (ip) with CLK1-IN-1 (25) (30 mg/kg), 30 (30 mg/kg, positive control), rapamycin (30 mg/kg, positive control), or solvent (12.5% ethanol and 12.5% castor oil, 10 mL/kg), immediately followed by APAP (500 mg/kg) injection (ip). All mice are sacrificed 6 h later. Liver sections are examined by H&E staining, and the serum from the blood samples is used for ALT and AST activity tests[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

409.42

Formula

C₂₄H₁₆FN₅O

CAS No.

2123491-32-5

SMILES

C[[email protected]@H](C1=CC=C(F)C=C1)N2N=NC3=C2C4=CC(C5=CC=C6C(N=CO6)=C5)=CC=C4N=C3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CLK1-IN-1
Cat. No.:
HY-103082
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CLK1-IN-1

Cat. No.: HY-103082