521064-34-6
Chemical Structure
CT 32228
- CAS No.: 521064-34-6
- Formula:C16H13BrClN5
- Molecular Weight:390.66
InChIKey: NUPGPJBRKLLVNK-UHFFFAOYSA-N
SMILES: ClC1=CC(C2=NC(NC3=CC=C(C=C3)Br)=NC(N)=N2)=C(C)C=C1
Biological Activity: CT 32228 is a selective LPAAT-β inhibitor with an IC50 of 60 nM. CT 32228 inhibits LPAAT-β-mediated acyl-CoA-dependent acylation of lysophosphatidic acid and lysophosphatidylmethanol in a non-competitive and isoform-specific manner, reducing phosphatidic acid and downstream oncogenic signaling. CT 32228 exerts antiproliferative and cytotoxic activity in tumor cell lines and multiple myeloma cells, inducing caspase-mediated apoptosis and cell cycle arrest. CT 32228 can be used for research on multiple myeloma, non-Hodgkin's lymphoma, and acute leukemia[1][2][3][4][5].
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CT 32228 | 95.27% | CT 32228 is a selective LPAAT-β inhibitor with an IC50 of 60 nM. CT 32228 inhibits LPAAT-β-mediated acyl-CoA-dependent acylation of lysophosphatidic acid and lysophosphatidylmethanol in a non-competitive and isoform-specific manner, reducing phosphatidic acid and downstream oncogenic signaling. CT 32228 exerts antiproliferative and cytotoxic activity in tumor cell lines and multiple myeloma cells, inducing caspase-mediated apoptosis and cell cycle arrest. CT 32228 can be used for research on multiple myeloma, non-Hodgkin's lymphoma, and acute leukemia. | ||||||||||||||||||||
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References
- [1]. Hollenback D, et al. Substrate specificity of lysophosphatidic acid acyltransferase β—evidence from membrane and whole cell assays. Journal of lipid research. 2006 Mar 1;47(3):593-604.
- [2]. Gong B, et al. Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta. Bioorg Med Chem Lett. 2004 May 3;14(9):2303-8. [Content Brief]
- [3]. Hideshima T, et al. Antitumor activity of lysophosphatidic acid acyltransferase-beta inhibitors, a novel class of agents, in multiple myeloma. Cancer Res. 2003 Dec 1;63(23):8428-36. [Content Brief]
- [4]. Pagel JM, et al. Induction of apoptosis using inhibitors of lysophosphatidic acid acyltransferase-beta and anti-CD20 monoclonal antibodies for treatment of human non-Hodgkin's lymphomas. Clin Cancer Res. 2005 Jul 1;11(13):4857-66. [Content Brief]
- [5]. Douvas MG, et al. Effect of lysophosphatidic acid acyltransferase-beta inhibition in acute leukemia. Leuk Res. 2006 Aug;30(8):1027-36. [Content Brief]