Description
CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC50 of 2 nM.
Product information
CAS Number: 2123491-32-5
Molecular Weight: 409.42
Formula: C24H16FN5O
Chemical Name: 5-{1-[(1S)-1-(4-fluorophenyl)ethyl]-1H-[1,2,3]triazolo[4,5-c]quinolin-8-yl}-1,3-benzoxazole
Smiles: C[C@@H](C1C=CC(F)=CC=1)N1N=NC2C=NC3=CC=C(C=C3C1=2)C1C=C2N=COC2=CC=1
InChiKey: BHKVSOQUPYXVRZ-AWEZNQCLSA-N
InChi: InChI=1S/C24H16FN5O/c1-14(15-2-6-18(25)7-3-15)30-24-19-10-16(4-8-20(19)26-12-22(24)28-29-30)17-5-9-23-21(11-17)27-13-31-23/h2-14H,1H3/t14-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (61.06 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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