LDC000067

製品コードS7461 バッチS746102

印刷

化学情報

Chemical Structure Synonyms LDC067 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H18N4O3S
分子量 370.43 CAS No. 1073485-20-7
Solubility (25°C)* 体外 DMSO 74 mg/mL (199.76 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]
特徴 CDK9-selective inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ In vitro enzymic kinase assay for CDKs
The FRET-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Kinase activity and inhibition in this assay is measured as recommended by the manufacturer. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the KM values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are recorded in a time-resolved manner in a Perkin Elmer EnVision reader.

カスタマーフィードバック

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

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

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Inhibition of CDK9 attenuates atherosclerosis by inhibiting inflammation and phenotypic switching of vascular smooth muscle cells [ Aging (Albany NY), 2021, 13(11):14892-14909] PubMed: 34102609

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。