NVP-LCQ195

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NVP-LCQ195

CAS No. : 902156-99-4

Biological Activity:NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
IC50 Value: 1 nM(CDK5/p25 and CDK5/p35); 2 nM(CDK1/cyclinB and CDK2/cyclinA); 5 nM(CDK2/cyclinE); 42 nM(CDK3/cyclinE)
Target: CDKs
LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-lmol/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. 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. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM.

Research Area:Cancer

Targets:CDK

Related Screening Libraries:Bioactive Compound Library Plus;Cell Cycle/DNA Damage Compound Library;Kinase Inhibitor Library;Anti-Cancer Compound Library;Anti-Aging Compound Library;Anti-Breast Cancer Compound Library;Anti-Pancreatic Cancer Compound Library;Anti-Blood Cancer Compound Library;Targeted Diversity Library;Cancer Stem Cells Compound Library;

Related Small Molecules:DB0614;Dinaciclib;SNS-032;CC-671;(E/Z)-Zotiraciclib;CDK1-IN-4;CCT-251921;BS-181;Samuraciclib hydrochloride hydrate;T025;Flavopiridol;CDK8-IN-3;CDK9-IN-12;FLT3/CDK4-IN-1;GFB-12811;GSK 3 Inhibitor IX;Eciruciclib;CDK-IN-6;Lerociclib dihydrochloride;CDK4/6-IN-13;ON-013100;(2S,3R)-Voruciclib hydrochloride;Cucurbitacin E;THZ1;CDK2-IN-14-d3;CDK7-IN-2 hydrochloride hydrate;MeBIO;BSJ-4-116;Cirtuvivint

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