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KU-177
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KU-177图片
CAS NO:1160952-43-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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凋亡 (apoptosis),可用于 Tau 病的研究。
生物活性

KU-177 is a potent inhibitor ofHsp90ATPase homologue 1 (Aha1), ablatesAha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disruptsAha1/Hsp90interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research[1][2].

IC50& Target

HSP90

 

体外研究
(In Vitro)

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.
体内研究
(In Vivo)

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 withBortezomib(HY-10227) (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.
分子量

489.47

Formula

C27H23NO8

CAS 号

1160952-43-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.