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.

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Selleck's LDC000067 has been cited by 33 publications

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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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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID