RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
体外研究
RIN1 inhibits the proliferation of hematologic cancer cell lines and promoted skeletal muscle diferentiation from C2C12 myoblasts.
RIN1 (0.6 µM, corresponding to 3 × IC50) decreases the number of MHC+ cells and increased the number of nuclei per cell, indicating that it induces the formation of multinucleated myofbers.
Cell Viability Assay
Cell Line:
AD-293 cells were transfected with RBPJ-VP16myc.
Concentration:
2 μM.
Incubation Time:
17 hours.
Result:
Inhibited Hes1-Luciferase activity with an IC50 of 0.18 µM and Emax of 82%.
Inhibited NOTCH3 ICD with similar potency and efcacy (0.19 µM and Emax=88%).
Cell Proliferation Assay
Cell Line:
T-cell acute lymphoblastic leukemia (T-ALL) patients (Jurkat and KOPT-K1) and in the mantle cell lymphoma (MCL) line REC-1.
Concentration:
0.1-10 μM.
Incubation Time:
96 h.
Result:
Inhibited NOTCH-dependent tumor cell proliferation.
Was active in both the cancer cell anti-proliferation and myoblast diferentiation assays.
运输条件
Room temperature in continental US; may vary elsewhere.