LDC000067

Catalog No.S7461 Batch:S746101

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Technical Data

Formula

C18H18N4O3S
Molecular Weight 370.43 CAS No. 1073485-20-7
Solubility (25°C)* In vitro DMSO 74 mg/mL (199.76 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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]
Features CDK9-selective inhibitor.

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/24102143/

Customer Product Validation

<p>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.</p>

, , Hum Mol Genet, 2017, 26(17):3421-3431

(B) Effects of siRNA-mediated depletion of CDK7, CDK9, or CDK7 and CDK9 on UKF-NB-3 and UKF-NB-3<sup>r</sup>SNS-032<sup>300nM</sup> cell viability as determined by MTT assay 72 h post-transfection. Non-targeting

Data from [ , , Oncotarget, 2016, 7(36):58051-58064 ]

Inhibition of JQ1 enhancement effect on Ad2 infection by CDK9 inhibitor. A549 cells were infected with Ad2 in the absence or presence of 300 nM JQ1. For inhibition, LDC00067 was added simultaneously. Viral protein synthesis or virion production was detected at 24 and 36 h PI, respectively. The experiments were performed 2 times independently. Data represent mean ± SD of triplicate samples. *p < 0.05, **p < 0.01.

Data from [ , , Sci Rep, 2018, 8(1):11554 ]

Western blotting after 24h of LDC000067 treatment, showing the expression of CDK9, RNA Pol II,phosphorylation of RNA Pol II (Ser2 and Ser5), anti-apoptotic proteins Mcl-1 and Survivin, and apoptotic-related protein Bax in (D)SYO-1 and (E) Fuji synovial sarcoma cells. The data are mean SD of the experiment carried out in triplicate.

Data from [ , , J Orthop Res, 2018, doi:10.1002/jor.24189 ]

Selleck's LDC000067 Has Been Cited by 44 Publications

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9] PubMed: 40449480
Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19] PubMed: 38218188
Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19] PubMed: 38218188
Excessive transcription-replication conflicts are a vulnerability of BRCA1-mutant cancers [ Nucleic Acids Research, 2023, 4341–4362] PubMed: None
Excessive transcription-replication conflicts are a vulnerability of BRCA1-mutant cancers [ Nucleic Acids Res, 2023, gkad172] PubMed: 36928661
Aberrant accumulation of Kras-dependent pervasive transcripts during tumor progression renders cancer cells dependent on PAF1 expression [ Cell Rep, 2023, 42(8):112979] PubMed: 37572321
The PAF1 complex promotes 3' processing of pervasive transcripts [ Cell Rep, 2022, 38(11):110519] PubMed: 35294889
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer [ Breast Cancer Res, 2022, 24(1):41] PubMed: 35715861
CDK9 inhibition blocks the initiation of PINK1-PRKN-mediated mitophagy by regulating the SIRT1-FOXO3-BNIP3 axis and enhances the therapeutic effects involving mitochondrial dysfunction in hepatocellular carcinoma [ Autophagy, 2021, 1-19] PubMed: 34890308
Probing the signaling requirements for naive human pluripotency by high-throughput chemical screening [ Cell Rep, 2021, 35(11):109233] PubMed: 34133938

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.