CB-5339

Research use only, not for human use.

p97-IN-1 is a potent inhibitor of p97 with an IC 50 <30 nM .

CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research. CB-5339 extracted from WO2015109285A1 compound FF07.

Western Blot AnalysisCell Line:MV4-11 AML cell line Concentration:0,0.2,0.4,0.8,1.6 μM Incubation Time:24-48 hours Result:Induced dose-dependent polyubiquitin protein accumulation at concentrations ≥ 0.4 μM. Induced the ER stress marker GRP78 accumulated at concentrations ≥ 0.4 μM. Induced spliced XBP-1 and ATF-4 accumulated after treatment with CB-5339 at concentrations ≥ 1.6 μM and 0.8 μM respectively arguing for a concentration-dependent increase in proteotoxic stress.

Animal Model:MLL-AF9-driven patient-derived xenograft (PDX) AML model in C57BL/6 male mice Dosage:90 mg/kg Administration:oral gavage (p.o.)Result:Decreased bone marrow leukemic infiltration and circulating leukemic cells.

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Others

Other Targets

p97

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1863952-15-1

412.49

C24H24N6O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (242.43 mM; Ultrasonic (<80°C)

CC=1N(C=2C(=C(C(N)=O)C=CC2)C1)C3=NC(NCC4=CC=CC=C4)=C5C(N3)=NCCC5

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(-20℃)

With Ice Pack

≥ 2 years