[CAS NO. 2123491-32-5] CLK1-IN-1
PRODUCTS SPECIFICATIONS [2123491-32-5]
DESCRIPTION [2123491-32-5]
Overview
| MDL | MFCD31692336 |
|---|---|
| Molecular Weight | 409.42 |
| Molecular Formula | C24H16FN5O |
| SMILES | C[C@@H](C1=CC=C(F)C=C1)N2N=NC3=C2C4=CC(C5=CC=C6C(N=CO6)=C5)=CC=C4N=C3 |
Summary
CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 ( CLK1 ) inhibitor, with an IC 50 of 2 nM.
IC50 & Target
|
CLK1 2 nM (IC 50 ) |
In Vitro
CLK1 is the most potently inhibited kinase (IC 50 : 2 nM). In addition to CLK1, only two kinases have an IC 50 value less than 100 nM, namely CLK2 (IC 50 : 31 nM) and CLK4 (IC 50 : 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 61.06 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution
