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CDK9 inhibitor

Catalog No.GC12871

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CDK9 inhibitor Chemical Structure

Cas No.: 1415559-43-1

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10mM (in 1mL DMSO)
$76.00
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5mg
$69.00
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10mg
$129.00
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50mg
$368.00
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100mg
$670.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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.

Background

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.

Chemical Properties

Cas No. 1415559-43-1 SDF
Chemical Name N-[5-[[6-[3-(1,3-dioxoisoindol-2-yl)phenyl]pyrimidin-4-yl]amino]-2-methylphenyl]methanesulfonamide
Canonical SMILES CC1=C(C=C(C=C1)NC2=NC=NC(=C2)C3=CC(=CC=C3)N4C(=O)C5=CC=CC=C5C4=O)NS(=O)(=O)C
Formula C26H21N5O4S M.Wt 499.54
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0018 mL 10.0092 mL 20.0184 mL
5 mM 0.4004 mL 2.0018 mL 4.0037 mL
10 mM 0.2002 mL 1.0009 mL 2.0018 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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