LDC000067

For research use only.

Catalog No.S7461 Synonyms: LDC067

33 publications

LDC000067 Chemical Structure

CAS No. 1073485-20-7

LDC000067 (LDC067) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.

Selleck's LDC000067 has been cited by 33 publications

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Biological Activity

Description LDC000067 (LDC067) 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]
Assay
Methods Test Index PMID
Western blot
CDK9 / RNAPII / p-RNAPII / MCL-1 / BIRC5; 

PubMed: 30579871     


(D) The expression of proteins involved in the CDK9-signaling pathway in the U2OS osteosarcoma cell line was examined by Western blotting after 48 h of LDC067 treatment. (E) Semiquantitative analysis of (D) densitometry relative to tubulin. The data represent the mean ± SE of the experiment carried out in triplicate. (F) The expression of proteins involved in the CDK9-signaling pathway in the KHOS osteosarcoma cell line was examined by Western blotting after 48 h of LDC067 treatment. (G) Semiquantitative analysis of (F) densitometry relative to tubulin. The data are mean ± SE of the experiment carried out in triplicate.

30579871

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
in solvent
Synonyms LDC067
Smiles COC1=CC=CC=C1C2=CC(=NC=N2)NC3=CC=CC(=C3)CS(=O)(=O)N

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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.

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID