NVP-LCQ195

SKU: orb1296228

Description

NVP-LCQ195 (AT9311) is a potent, selective small-molecule inhibitor of cyclin-dependent kinases 1, 2, 3, and 5 with IC50 values in the low nanomolar range. It is a valuable research tool for studying cell cycle progression, neuronal function, and apoptosis in vitro, and has been utilized in preclinical cancer research models.

Research Area

Cell Biology

Key Properties

• CAS Number: 902156-99-4
• MW: 460.33
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₉Cl₂N₅O₄S
• SMILES: CS(=O)(=O)N1CCC(CC1)NC(=O)c1[nH]ncc1NC(=O)c1c(Cl)cccc1Cl
• Target: CDK
• Solubility: DMSO:100 mg/mL (217.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.69 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  CDK6-CyclinD3:187 nM|CDK5-p35:1 nM|CDK2-CyclinE:5 nM|CDK5-p25:1 nM|CDK2-CyclinA:2 nM|CDK3-CyclinE:42 nM|CDK7-CyclinH-MAT1:3564 nM|CDK9-CyclinT1:15 nM|CDK1-CyclinB:2 nM
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• In Vivo:
  Bortezomib-treated MM patients whose tumours had high baseline expression of genes suppressed by LCQ195 had significantly shorter progression-free and overall survival than those with low levels of these transcripts in their MM cells.
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• In Vitro:
  NVP-LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-1 mol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. In MM cells, LCQ195 triggered decreased amplitude of transcriptional signatures associated with oncogenesis, drug resistance and stem cell renewal, including signatures of activation of key transcription factors for MM cells e.g. myc, HIF-1a, IRF4.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AT 9311, AT9311, AT-9311, CDK5, CDK2, CDK3, CDK1, CDK, Cyclin dependent kinase, LCQ 195, LCQ195, LCQ-195, Inhibitor, inhibit, NVP LCQ195, NVP-LCQ 195, NVPLCQ195, NVP-LCQ195, NVP-LCQ-195

Compound Identifiers

PubChem CID

11655534