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编 号：F742802
分子式：C27H23NO8
分子量：489.47
分子式：C27H23NO8
分子量：489.47
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CAS No: 1160952-43-1
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生物活性：
KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research.
体内研究：
KU-177 (1 mg/kg; i.p.; twice a week; 4 weeks), inhibits tumor growth and extends the survival of 5TMM3VT MM mice without significant toxicity. KU-177 shows stronger efficacy in vivo, combined with Bortezomib (HY-10227) (1 mg/kg; i.p.).Animal Model:5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice)
Dosage:1 mg/kg
Administration:Intraperitoneal injection; twice a week; sacrificed mice with hindlimb weakness immediately, about 4-5 weeks
Result:Inhibited the xenograft tumor growth of both ANBL6 WT/BTZ-DR cells.Didn’t induce histopathological abnormities or lesions in main organs including heart, liver, spleen, lung and kidney.
体外研究：
KU-177 (50 μM; 48 h) hampers the proliferation of flow MRD-positive cells in both primary multiple myeloma (MM) and recurrent MM patient samples.KU-177 (30 μM; 48 h) inhibits proteasome activity in AHSA1 WT/OE cells, PSMD2 WT/OE cells and ANBL6 WT/DR cells.KU-177 abrogates the cellular proliferation and PI resistance induced by elevated AHSA1, and decreases the expression of CDK6 and PSMD2.KU-177 (25 μM; 30 min; 37 ℃) inhibits recombinant P301L tau aggregation without inhibiting Hsp90 to refold luciferase.KU-177 (10 μM; 24 h) exhibits the ability to disrupt interactions between Aha1 and Hsp90 inSH-SY5Y neuroblastoma cells and SK-BR-3 breast cancer cells, without significantly inhibition on Hsp90 client protein (Her2).
KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research.
体内研究：
KU-177 (1 mg/kg; i.p.; twice a week; 4 weeks), inhibits tumor growth and extends the survival of 5TMM3VT MM mice without significant toxicity. KU-177 shows stronger efficacy in vivo, combined with Bortezomib (HY-10227) (1 mg/kg; i.p.).Animal Model:5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice)
Dosage:1 mg/kg
Administration:Intraperitoneal injection; twice a week; sacrificed mice with hindlimb weakness immediately, about 4-5 weeks
Result:Inhibited the xenograft tumor growth of both ANBL6 WT/BTZ-DR cells.Didn’t induce histopathological abnormities or lesions in main organs including heart, liver, spleen, lung and kidney.
体外研究：
KU-177 (50 μM; 48 h) hampers the proliferation of flow MRD-positive cells in both primary multiple myeloma (MM) and recurrent MM patient samples.KU-177 (30 μM; 48 h) inhibits proteasome activity in AHSA1 WT/OE cells, PSMD2 WT/OE cells and ANBL6 WT/DR cells.KU-177 abrogates the cellular proliferation and PI resistance induced by elevated AHSA1, and decreases the expression of CDK6 and PSMD2.KU-177 (25 μM; 30 min; 37 ℃) inhibits recombinant P301L tau aggregation without inhibiting Hsp90 to refold luciferase.KU-177 (10 μM; 24 h) exhibits the ability to disrupt interactions between Aha1 and Hsp90 inSH-SY5Y neuroblastoma cells and SK-BR-3 breast cancer cells, without significantly inhibition on Hsp90 client protein (Her2).
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