lcl161 Inhibitor CAS No. 1005342-46-0

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Chemical Characteristic

Product Name	lcl161
CAS No.	1005342-46-0
Molecular Weight	500.63
Formula	C₂₆H₃₃FN₄O₃S
Chemical Name	(S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(methylamino)propanamide
Smiles	C(=O)([C@@H](NC)C)NC(C(=O)N1[C@@H](CCC1)c1scc(n1)C(=O)c1ccc(cc1)F)C1CCCCC1
Chemical Structure

Biological activities

LCL161 is a small molecule mimetic of the second mitochondria-derived activator of caspases (SMAC) that is an inhibitor of inhibitors of apoptosis (IAP). LCL161 binds to IPAs and initiates the destruction of the cellular inhibitor of apoptosis 1 and 2. LCL161 induces apoptosis in vitro and potentiates the effects of tyrosine kinase inhibition against leukemic disease. In vitro, LCL161 achieves 50% growth inhibition in cell lines including COG-LL-317, CCRF-CEM and Karpas-299, with CCRF-CEM and Karpas-299 showing IC50 values of 0.25 and 1.6µM, respectively.^[1] LCL161 induces cytotoxicity and apoptosis in cells that express lower levels of Bcl-2 such as PLC5 and Hep3B and but no in cells with higher Bcl-2 expression such as Huh-7 and SK-Hep1. Down regulation of Bcl-2 by small interference RNA overcomes the resistance to LCL161 in Huh-7.^[2] In in vivo tests, LCL161 induces significant tumor growth delay in multiple solid tumor panels, such as osteosarcoma, glioblastoma and neuroblastoma panels.^[1]

Protocols

LCL161 is dissolved in 0.1N HCl and diluted to volume with sodium acetate buffer(100mM, pH 4.63) to produce a solution with pH 4.3-4.6.^[1]

References

[1] Houghton PJ, Kang MH, Reynolds CP, Morton CL, Kolb EA, Gorlick R, Keir ST, Carol H, Lock R, Maris JM, Billups CA, Smith MA. Initial testing (stage 1) of LCL161, a SMAC mimetic, by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2012, 58(4):636-639. [2] Chen KF, Lin JP, Shiau CW, Tai WT, Liu CY, Yu HC, Chen PJ, Cheng AL. Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells. Biochem Pharmacol. 2012, 84(3):268-277.

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