OTUB1/USP8-IN-1

Research use only, not for human use.

OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8.

OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer.

OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) has antiproliferative effects in KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines.OTUB1/USP8-IN-1 (500 nM; 24 h) decreases in protein levels of both UBE2N and EGFR in H1975 cells.Cell Viability Assay Cell Line:KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines Concentration:10 nM-10 μM Incubation Time:72 hours Result:Inhibited cell proliferative with IC50 values of 118, 145, 172, 431, and 1004 nM for H1975, H1703, EBC-1, H23, and A549 cells, respectively.Western Blot Analysis Cell Line:H1975 cells Concentration:500 nM Incubation Time:24 hours Result:Decreased the levels of both UBE2N and EGFR in a dose-dependent manner.

OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model.Animal Model:Female BALB/c nude mice with H1975 xenografts (5 weeks of age) Dosage:5 mg/kg Administration:Intraperitoneal injection; QD and BID, for 2 weeks Result:Reduced total tumor weight and average tumor volume in an over twofold with BID dosing.Animal Model:Female BALB/c nude mice with H1975 xenograft (5 weeks of age) Dosage:1 and 10 mg/kg Administration:Intravenous injection (1 mg/kg) and oral administration (10 mg/kg).

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Proteasome/Ubiquitin

DUB

DUB

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2858800-98-1

426.83

C22H16ClFN2O4

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (117.15 mM; Ultrasonic )

O=C1C2=C(OC(=N2)C3=C(Cl)C(O[C@H]4CN(C)CC4)=CC=C3F)C(=O)C=5C1=CC=CC5

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(-20℃)

With Ice Pack

≥ 2 years