MKC8866

Research use only, not for human use.

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro).

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

MKC8866 (20μM; 6 days) decreases proliferation of all breast cancer cell lines.MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase.MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells.MKC8866 (20 μM; 72hours) is sufficient to completely block NSC 125973-induced expression of XBP1s . Cell Proliferation Assay Cell Line:MCF7, SKBR3, MDA-MB-231 and MCF10A cells Concentration:20?μM Incubation Time:For 6 days Result:Decreased proliferation of all breast cancer cell lines.Cell Cycle Analysis Cell Line:MDA-MB-231, MCF7 and SKBR3 cells Concentration:20?μM Incubation Time:48 hours Result:Reduced the number of cells entering S phase.Cell Cycle Analysis Cell Line:LNCaP, VCaP, 22Rv1 and C4-2B cells Concentration:0.2, 0.5, 1, 5, 10 μM Incubation Time:3 days Result:Suppressed the viability of all four cell lines in a dose-dependent manner.Cell Cycle Analysis Cell Line:MDA-MB-231 cells Concentration:20 μM Incubation Time:72? hours Result:Completely blocked NSC 125973-induced expression of XBP1s.

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal. Animal Model:Female athymic nude mice with MDA-MB-231 tumor Dosage:300 mg/kg Administration:Oral; for 28 days Result:Reduced tumor regrowth post-NSC 125973 withdrawal.

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Others

Other Targets

IRE1 RNase

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1338934-59-0

361.35

C18H19NO7

>98% (HPLC)

DMSO:16.67 mg/mL (46.13 mM; Need ultrasonic)

O=CC1=C(O)C(OC)=CC2=C1OC(C(CC(N3CCOCC3)=O)=C2C)=O

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(-20℃)

With Ice Pack

≥ 2 years