LDC000067

Catalog No.S7461 Synonyms: LDC067

LDC000067 Chemical Structure

Molecular Weight(MW): 370.43

LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

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2 Customer Reviews

  • Inhibition of CDK9 leads to a decrease in RNApol II activity and repetitive element expression. HEK293T cells were treated with DMSO control and the indicated amounts of LDC000067, a CDK9 inhibitor, for a total of 3 h. (A) Immunoblots showing the levels of phosphorylated RNApol II largest subunit (pRPB1), total RPB1 and GAPDH, in response to different doses of CDK9 inhibitor. (B) Quantification of immunoblots from 2 independent experiments in which each condition was performed in duplicates, and in which pRPB1 and total RPB1 protein levels were normalized to GAPDH or as pRPB1/Total RPB1 ratio. (C, D) qRT-PCR analyses show a significant response to CDK9 inhibition of repetitive elements belonging to the LTR (C) and SINE (D) classes. Statistical analyses were performed to compare all groups using a One-way ANOVA followed by Bonforreoni’s multiple comparison test, *P < 0.05, **P < 0.01, #P < 0.0001.

    Hum Mol Genet, 2017. LDC000067 purchased from Selleck.

    (B) Effects of siRNA-mediated depletion of CDK7, CDK9, or CDK7 and CDK9 on UKF-NB-3 and UKF-NB-3rSNS-032300nM cell viability as determined by MTT assay 72 h post-transfection. Non-targeting 'scrambled' siRNA (scr siRNA) served as control.

    Oncotarget, 2016, 7(36):58051-58064. LDC000067 purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description LDC000067 is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.
Features CDK9-selective inhibitor.
Targets
CDK9 [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
44 nM 2.441 μM
In vitro

LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo RNA synthesis of cellular genes.[1]

Protocol

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.76 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 370.43
Formula

C18H18N4O3S

CAS No. 1073485-20-7
Storage powder
Synonyms LDC067

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID