RGNCY-0105 (TCB CaMKIIgamma inhibitor)

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TCB (tosyl chloride-berbamine) is a novel, orally active small molecule that efficiently eliminates-positive leukemia in vitro and in vivo.  TCB significantly reduces MYC protein by inhibiting CaMKIIwhich is an enzyme critical in stabilizing MYC protein, and induces apoptosis of MYC-positive leukemia cells.  Oral administration of TCB in vivo, significantly eliminated lethal MYC-positive acute lymphoblastic leukemia (ALL) in the orthotopic muse model.  These data demonstrate that TCB is an excellent inhibitor targeting the CaMKIIg/Myc axis for treating MYC-mediated leukemia.

Systematic Name:  (11S,31R)-16,36,37-trimethoxy-12,32-dimethyl-11,12,13,14,31,32,33,34-octahydro-2,6-dioxa-1(7,1),3(8,1)-diisoquinolina-5(1,3),7(1,4)-dibenzenacyclooctaphane-54-yl 4-methylbenzenesulfonate


Formula: C44H46N2O8

Mol Wt:  762.92

PMID:  31247466

Tags: Leukemia, Apoptosis, small molecule, Myc, ALL, RGNCY-0105, TCB, CaMKII, CaMKIIgamma