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Technical Data
| Formula | C18H18N4O3S |
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| 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 | |||
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* <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.) |
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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. | ||||
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| 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)
Customer Product Validation
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, , Hum Mol Genet, 2017, 26(17):3421-3431
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Data from [Data independently produced by , , Oncotarget, 2016, 7(36):58051-58064]
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Data from [Data independently produced by , , Sci Rep, 2018, 8(1):11554]
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Data from [Data independently produced by , , J Orthop Res, 2018, doi:10.1002/jor.24189]
Selleck's LDC000067 has been cited by 43 publications
| 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 |
| Novel CDK9 inhibitor oroxylin A promotes wild-type P53 stability and prevents hepatocellular carcinoma progression by disrupting both MDM2 and SIRT1 signaling [ Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00708-2] | PubMed: 34188177 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.