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Alternative_name
CAY10574; UNII-ZG0O47K626; ZG0O47K626; CAN508; 4-(3,5-Diamino-1H-pyrazol-4-ylazo)-phenol; 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol; 3,5-diamino-4-(4-hydroxyphenyl)azopyrazole; 4-Arylazo-3,5-diamino-1H-pyrazole 31b
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Description
Cdk9 Inhibitor II is a potent and selective inhibitor of Cdk9 with an IC₅₀ value of 0.35 µM in vitro. It is also an inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC₅₀ values of 13.3 µM and 20 µM respectively. It reduces the frequency of S-phase cells in the cancer cell line HT-29 and decreases the phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II. It inhibits mRNA synthesis and induces the tumor suppressor protein p53. It inhibits cell proliferation of cancer cell lines such as MCF-7, HOS, G361, and K562 cells with IC₅₀ values of 33 µM, 49 µM, 64 µM, and 62 µM respectively.
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CAS Number
140651-18-9
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Structure Available
True
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Salt Form
false
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Molecular Formula
C₉H₁₀N₆O
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Molecular Weight
218.22
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Cell Permeable
True
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Purity
≥95%
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Solubilities
~0.5 mg/ml in DMSO and DMF in 0
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Handling
Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
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Tag Line
A selective inhibitor of Cdk9
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Storage Condition
-20ºC
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Shipping Condition
RT
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Shelf Life
36months
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MDL Number
MFCD09262258
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PubChem CID
135398514
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SMILES
C1=CC(=CC=C1N=NC2=C(NN=C2N)N)O
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InChi
InChI=1S/C9H10N6O/c10-8-7(9(11)15-14-8)13-12-5-1-3-6(16)4-2-5/h1-4,16H,(H5,10,11,14,15)
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MSDS Available
True
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
