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CDK9 inhibitor

In stock
Catalog No.
A3294
CDK9 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$140.00
In stock
5mg
$127.00
In stock
10mg
$241.00
In stock
50mg
$686.00
In stock
100mg
$1,248.00
In stock

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CDK9 inhibitor is a small-molecule selective inhibitor of CDK9 (cyclin dependent kinase 9) with IC50 value of 39 nM [1].
CDKs are a group of serine/threonine kinases and are widely spread in all known eukaryotes. CDKs are activated through binding to cyclins and forming heterodimers. In the dimer, CDK acts as a catalytic subunit and phosphorylates the down-stream proteins such as nuclear lamina protein, nucleolin and histone H1. Through this way, CDKs take participate in the cell cycle regulation. CDK9 is a special member of the CDK family. It can affect the elongation phase of transcription through phosphorylating RNA polymerase II. The partner of it is positive elongation factor b (P-TEFb). It is reported that CDK9 is necessary for the infection of many kinds of viruses such as HIV-1 and HSV1 [1].
CDK9 inhibitor is a 4-aminophenyl derivative based on the (6-phenyl-pyrimidin-4-yl)-phenylamine structure. It showed elevated selectivity against CDK9 than the previous found inhibitors. The IC50 values of CDK9 inhibitor for CDK1/CycB, CDK2/CycE, CDK3/CycE, CDK4/CycD1, CDK5/p35, CDK6/CycD1 and CDK7/CycH are all higher than 1 μM. CDK9 inhibitor has no cytotoxicity. The treatment of CDK9 inhibitor at concentrations of 1 μM and 2 μM resulted in the cell viabilities of 101% and 115%, respectively. It also showed no significant toxicity in H9 cells. In the p24 assay, CDK9 inhibitor exerted its potency in inhibiting HIV-1 propagation with about 10% reduction of p24 production [1].
References:
1.Németh G, Varga Z, Greff Z, et al. Novel, selective CDK9 inhibitors for the treatment of HIV infection. Curr Med Chem, 2011;18(3):342-58.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt499.54
Cas No.1415559-43-1
FormulaC26H21N5O4S
SolubilitySoluble in DMSO
Chemical NameN-[5-[[6-[3-(1,3-dioxoisoindol-2-yl)phenyl]pyrimidin-4-yl]amino]-2-methylphenyl]methanesulfonamide
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)NC2=NC=NC(=C2)C3=CC(=CC=C3)N4C(=O)C5=CC=CC=C5C4=O)NS(=O)(=O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

MT4 cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

2.5 μM; 1 week

Applications

In HIV-1 infected MT4 cells, CDK9 Inhibitor at 2.5 μM potently inhibited HIV-1 propagation due to positive elongation factor b (P-TEFb) inhibition. Moreover, in MT4 cells, CDK9 Inhibitor at the concentrations of 1 μM and 2 μM resulted in the cell viabilities of 101% and 115%, respectively, which implied CDK9 Inhibitor had no cytotoxicity. In the p24 assay, CDK9 Inhibitor down-regulated the expression of p24 protein by 10%.

References:

[1]. Németh G, Varga Z, Greff Z, et al. Novel, selective CDK9 inhibitors for the treatment of HIV infection. Curr Med Chem, 2011;18(3):342-58.

Quality Control

Quality Control & MSDS

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Chemical structure

CDK9 inhibitor

Related Biological Data

CDK9 inhibitor