219511
Cdc2-Like Kinase Inhibitor IV, KH-CB19
The Cdc2-Like Kinase Inhibitor IV, KH-CB19 controls the biological activity of Cdc2-Like KInase. This small molecule/inhibitor is primarily used for Cell Structure applications.
동의어(들):
Cdc2-Like Kinase Inhibitor IV, KH-CB19, ( E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV, (E)-Ethyl-3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate, Clk Inhibitor IV
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크기 선택
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제품정보 (DICE 배송 시 비용 별도)
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
ClC1=C(Cl)C(N(C)C(C(OCC)=O)=C2/C(C#N)=C\N)=C2C=C1
General description
A cell-permeable N-methylindolyl-enaminonitrile that acts as a more potent inhibitor than TG003 (Cat. No. 219479) against CLK1 activity (IC50 = 19.7 and 48.6 nM, respectively) by targeting the kinase ATP binding site in a non-ATP mimetic fashion. KH-CB19 is also reported to exhibit higher potency than TG003 against DYRK1A (IC50 = 55.2 vs. 156.1 nM, respectively) and CLK3 (IC50 = 0.53 vs. >4 µM, respectively), while exhibiting no activity against a panel of 71 other protein kinases. Thermostability shift assay reveals stronger interaction of KH-CB19 toward CLK4 than CLK1, predicting better or at least comparable potency against CLK4. KH-CB19 is shown to be more effective than TG003 in suppressing both basal and TNF-α-stimulated phosphorylation of serine/arginine rich proteins SRp55 (77.5% vs. 45% inhibition by 5 µM respective inhibitor against stimulated level) and SRp75 (80% vs. 27.5% inhibition by 5 µM respective inhibitor against stimulated level), as well as human tissue factor spliced variants, flTF and asHTF, mRNA levels in human microvascular endothelial cells HMEC-1.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Fedorov, O., et al. 2011. Chem. Biol.18, 67.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.