2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis Autophagy
  3. HSP Apoptosis Autophagy ULK RIP kinase CDK
  4. VWK147

VWK147 是一种第二代 HSP90 C-末端结构域 (CTD) 抑制剂。VWK147 作用于 CTD 二聚化界面，阻止 HSP90 CTD 二聚化，破坏共伴侣蛋白 PPID 与 HSP90 CTD 的结合，并抑制依赖于二聚化的 HSP90 潜在功能。VWK147 降低 HSP90 客户蛋白 ULK1、RIPK1 和 CDK4 的蛋白水平，且不诱导热休克反应。VWK147 在 Cisplatin (HY-17394) 敏感和耐药的尿路上皮癌细胞中诱导细胞死亡，包括凋亡 (apoptosis)。VWK147 诱导 LC3-II 积累，抑制自噬体-溶酶体融合以阻断经典自噬 (autophagy)，并诱导不依赖于 ULK1 和 PIK3C3 复合物的非经典 LC3 脂化。VWK147 可用于尿路上皮癌的研究。

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VWK147

VWK147 Chemical Structure

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VWK147 相关抗体

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma[1].

IC50 & Target

HSP90

 

ULK1

 

CDK4

 

RIPK1

 

体外研究
(In Vitro)

VWK147 在 TR-FRET 实验中可抑制 HSP90β CTD 与 PPID 之间的相互作用[1]。
VWK147 (10 μM；3 h) 在荧光偏振实验中不与 HSP90 NTD 结合[1]。
VWK147 (25-100 μM；作用 1 小时) 在无细胞荧光素酶复性实验中抑制 HSP90 的分子伴侣功能[1]。
VWK147 (2-50 μM；孵育 1 小时) 可在 BS3 交联剂实验中减少 HSP90α CTD 二聚体[1]。
VWK147 (1-10 μM；作用 6 小时) 可在 Cisplatin 敏感型 T24 和 Cisplatin 耐药型 T24-CR 尿路上皮癌细胞中破坏 HSP90 的客户蛋白 ULK1、RIPK1 及 CDK4 的稳定性[1]。
VWK147 (0.1-100 μM；作用 72 小时) 可降低 Cisplatin 敏感型 (253J、T24) 和耐药型 (253J-CR、T24-CR) 尿路上皮癌细胞的细胞活力，作用 72 小时后的 IC50 值约为 3-5 μM[1]。
VWK147 (10 μM；0-24 h) 可在 24 小时内诱导 T24 和 T24-CR 尿路上皮癌细胞发生兼具凋亡和坏死特征的细胞死亡[1]。
VWK147 (5 μM；作用 24 h) 在 253J、253J-CR、T24 及 T24-CR 尿路上皮癌细胞中诱导的细胞死亡呈半胱天冬酶 (caspase) 部分依赖性[1]。
VWK147 (1-10 μM；处理 6 小时) 可在 T24 和 T24-CR 尿路上皮癌细胞中诱导浓度依赖性的 PARP1 切割[1]。
VWK147 (5 μM；1-24 h) 可在 24 小时内以时间依赖的方式诱导 T24 和 T24-CR 尿路上皮癌细胞中的 PARP1 剪切[1]。
VWK147 (5 μM；0-24 h) 可在 24 小时内诱导 Cisplatin 敏感型 (253J、T24) 和 Cisplatin 耐药型 (253J-CR、T24-CR) 尿路上皮癌细胞中的 caspase-3 活化[1]。
VWK147 (5 μM；6 h) 可抑制 T24 和 T24-CR 尿路上皮癌细胞中的自噬流，表现为 LC3-II 的累积[1]。
VWK147 (5 μM；4 h) 可在稳定表达 mRFP-EGFP-rLC3 的 T24 和 T24-CR 尿路上皮癌细胞中抑制自噬体-溶酶体的融合[1]。

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

VWK147 相关抗体:

Western Blot Analysis[1]

Cell Line: Cisplatin-sensitive (T24) and -resistant (T24-CR) urothelial carcinoma cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 6 h
Result: Reduced levels of HSP90 client proteins ULK1, RIPK1, and CDK4 in both T24 and T24-CR cells.\nDid not increase levels of HSP27, HSP40, or HSP70.

Cell Viability Assay[1]

Cell Line: Cisplatin-sensitive (253J, T24) and -resistant (253J-CR, T24-CR) urothelial carcinoma cells
Concentration: 0.1-100 μM
Incubation Time: 72 h
Result: Reduced cell viability in all four cell lines with IC50 values of ~3-5 μM for 253J, ~3-5 μM for 253J-CR, ~3-5 μM for T24, and ~3-5 μM for T24-CR.

Cell Viability Assay[1]

Cell Line: 253J, 253J-CR, T24, and T24-CR urothelial carcinoma cells
Concentration: 5 μM (with 20 μM Q-VD-OPh (HY-12305) as co-treatment)
Incubation Time: 24 h
Result: Had its mediated cell viability reduction partially reduced by Q-VD-OPh but not abolished, indicating partial pro-apoptotic effects.

Western Blot Analysis[1]

Cell Line: T24 and T24-CR urothelial carcinoma cells
Concentration: 1-10 μM
Incubation Time: 6 h
Result: Increased cleaved PARP1 levels in a concentration-dependent manner in both cell lines.

Western Blot Analysis[1]

Cell Line: T24 and T24-CR urothelial carcinoma cells
Concentration: 5 μM
Incubation Time: 1-24 h
Result: Induced time-dependent PARP1 cleavage, with increased cleavage over 24 h.

Western Blot Analysis[1]

Cell Line: T24 and T24-CR urothelial carcinoma cells
Concentration: 5 μM (with 20 nM bafilomycin A1 as co-treatment)
Incubation Time: 6 h
Result: Increased LC3-II levels with mono-treatment, but combination with Bafilomycin A1 did not further increase LC3-II levels, indicating inhibited autophagic flux; p62 levels were unaffected.

Immunofluorescence[1]

Cell Line: T24 and T24-CR cells stably expressing mRFP-EGFP-rLC3
Concentration: 5 μM
Incubation Time: 4 h
Result: Resulted in almost complete co-localization of GFP and RFP signals (yellow structures), indicating inhibited autophagosome-lysosome fusion (no red-only puncta).

Immunofluorescence[1]

Cell Line: T24 and T24-CR urothelial carcinoma cells
Concentration: 5 μM (with 5 μM SAR405 as co-treatment)
Incubation Time: 4 h
Result: Induced LC3-positive aggregates that were unaffected by SAR405, indicating PIK3C3-independent (non-canonical) LC3 lipidation.
分子量

674.71

Formula

C32H38N10O7
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

VWK147 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VWK147VWK 147VWK-147HSPApoptosisAutophagyULKRIP kinaseCDKHeat shock proteinsUnc-51 like kinaseReceptor-interacting protein kinasesRIPKCyclin dependent kinaseRIPK1PPIDurothelial carcinoma cellsautophagosome-lysosome fusionPIK3C3 complexesCDK4apoptosisHSP90 C-terminal domainmTOR inhibitorsULK1Inhibitorinhibitorinhibit

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