1. Product Overview
JSH-150 (CAS 2247481-21-4), systematically named 4-(((4-(5-Chloro-2-((trans-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile, is a potent and highly selective cyclin-dependent kinase 9 (CDK9) inhibitor. With the molecular formula C₂₄H₃₃ClN₆O₂S and a molecular weight of 505.08 g/mol, it appears as a light yellow to yellow solid at room temperature. JSH-150 inhibits CDK9 with an IC₅₀ of 1 nM in cell-free assays and effectively suppresses CDK9-dependent RNA polymerase II phosphorylation and MCL1 expression in cells. It also serves as a tool compound to study JAK2 bypass/STAT3 activation mechanisms in myeloproliferative neoplasms. This product is supplied exclusively for laboratory research use and is not intended for clinical, diagnostic, veterinary, food, or cosmetic applications.
2. Key Features and Advantages
• Ultra-high potency: Selective CDK9 inhibitor with IC₅₀ = 1 nM (cell-free); >1,000-fold selectivity over other CDKs (CDK1/2/4/6) and broad kinase panel.
• Clear mechanistic readout: Rapidly reduces phospho-RNA Pol II (Ser2) and MCL1 protein levels in tumor cell lines, enabling clean transcriptional/CDK9-dependency assays.
• High purity: Typically ≥98% by HPLC (suppliers also offer 99.96% by area), suitable for Western blot, qPCR, and cell viability studies.
• Good solubility: Readily soluble in DMSO (≥100 mg/mL = ~198 mM), enabling convenient high-concentration stock preparation (e.g., 10 mM or 50 mM in anhydrous DMSO).
• Consistent batch quality with supporting analytical data (HPLC, LC-MS, NMR) available from qualified suppliers; referenced in studies on MCL1-dependent cancers and JAK2-independent STAT3 activation.
• Stable under recommended storage; light yellow solid that maintains activity when protected from light and moisture.
3. Main Applications
• Oncology transcription research: Evaluating CDK9 inhibition on RNA Pol II phosphorylation, MCL1 downregulation, and apoptosis induction in AML, lymphoma, and solid tumors with high MCL1 dependence.
• Cell-based assays: Western blot for p-RNA Pol II (Ser2) and MCL1; qPCR for immediate-early gene expression; viability/proliferation in MV4-11, RS4;11, and other CDK9-sensitive lines.
• JAK2 bypass / myeloproliferative neoplasm models: Used to probe STAT3 activation independent of JAK2 (e.g., in JAK2V617F-mutant contexts where JSH-150 blocks STAT3 via CDK9).
• Medicinal chemistry reference: Serves as a structurally distinct CDK9 inhibitor compared to ATP-competitive tool compounds (e.g., SNS-032, THAL-SNS-032 PROTAC counterpart).
• General research use as a selective CDK9 probe in epigenetic and transcriptional regulation programs.
4. Technical Specifications
5. Storage and Handling
• Store the powdered compound sealed with desiccant, protected from light; recommended storage at -20°C (long term stable for 2–3 years). For DMSO stock solutions, prepare fresh or aliquot and store at -80°C (6 months stable) or -20°C (1 month); avoid repeated freeze–thaw cycles. Typical working stocks are 10 mM or 50 mM in anhydrous DMSO.
• Before opening, allow the sealed vial to warm to room temperature to prevent moisture condensation. Keep container tightly closed when not in use.
• Handle in a well-ventilated area or fume hood. Use personal protective equipment including safety glasses, nitrile gloves, and a lab coat. Avoid inhalation of dust and contact with skin or eyes.
• Intended exclusively for laboratory research by qualified personnel; not for human or veterinary use, food, drug, or cosmetic applications.
6. Safety Overview
• JSH-150 is a research chemical CDK9 inhibitor with limited toxicological data. Treat as potentially hazardous: may cause irritation to eyes, skin, and respiratory system.
• In case of eye contact, rinse immediately with plenty of running water for at least 15 minutes and seek medical advice. In case of skin contact, wash thoroughly with soap and water.
• If inhaled, move the person to fresh air and keep at rest in a position comfortable for breathing. If ingested, rinse mouth and seek medical attention—do not induce vomiting unless directed by medical personnel.
• Use appropriate engineering controls (fume hood) and personal protective equipment (safety goggles, nitrile gloves, lab coat). Avoid generating dust.
• Dispose of in accordance with local regulations for chemical waste. Do not discharge into drains, waterways, or soil.
• For detailed safety information, refer to the applicable Safety Data Sheet (SDS) prior to handling.
