KU-177 是HSP90ATP 酶同系物 1 (Aha1) 的有效抑制剂，可消融Aha1驱动的HSP90依赖性 tau 聚集增强。KU-177 还干扰Aha1/HSP90相互作用 (IC50=4.08 μM)，但不影响HSP90的再折叠荧光素酶的能力。KU-177 抑制癌细胞生长并诱导Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)，可用于 Tau 病的研究。

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 ( IC 50 =4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research [1] [2].

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 [1]. KU-177 (30 μM; 48 h) inhibits proteasome activity in AHSA1 WT/OE cells, PSMD2 WT/OE cells and ANBL6 WT/DR cells [1]. KU-177 abrogates the cellular proliferation and PI resistance induced by elevated AHSA1, and decreases the expression of CDK6 and PSMD2 [1]. KU-177 (25 μM; 30 min; 37 ℃) inhibits recombinant P301L tau aggregation without inhibiting Hsp90 to refold luciferase [2]. KU-177 (10 μM; 24 h) exhibits the ability to disrupt interactions between Aha1 and Hsp90 in SH-SY5Y neuroblastoma cells and SK-BR-3 breast cancer cells, without significantly inhibition on Hsp90 client protein (Her2) [2]. Cell Proliferation Assay [1] Cell Line: ARP1 and H929 WT and AHSA1-OE cells Concentration: 1 nM-100 μM Incubation Time: 24, 48, 72 hours Result: Decreased multiple myeloma (MM) cell proliferation and PI resistance induced by AHSA1/HSP90 in vitro. Cell Proliferation Assay [2] Cell Line: SH-SY5Y neuroblastoma cells and Her2 overexpressing SK-BR-3 breast cancer cells Concentration: 10 μM Incubation Time: 24 hours Result: Didn’t induce the degradation of Hsp90 client proteins Her2 (in SK-BR-3 cells), Cdk6, or pAktS473 (in SHSY5Y cells), nor induced the expression of Hsp70, a marker of the heat shock response.

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 (1 mg/kg; i.p.) [1]. Animal Model: 5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice) [1] 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.

1160952-43-1

C27H23NO8

489.47

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years