2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. KU-177

KU-177 是 Hsp90 ATP 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。

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KU-177 Chemical Structure

KU-177 Chemical Structure

CAS No. : 1160952-43-1

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KU-177 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KU-177 相关抗体:

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 with Bortezomib (HY-10227) (1 mg/kg; i.p.)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

KU-177 相关分类

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Keywords:

KU-1771160952-43-1KU177KU 177HSPHeat shock proteinsTauAmideproteostasisneurodegenerationARP1H929AHSA1-OE cellsSH-SY5Yneuroblastoma cellsHer2SK-BR-3breast cancer cellsInhibitorinhibitorinhibit

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