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

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.

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VWK147

VWK147 Chemical Structure

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VWK147 Related Antibodies

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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ULK1 ULK2

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RIPK1 RIPK2 RIPK3

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

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

 

In Vitro

VWK147 inhibits the interaction between HSP90β CTD and PPID in a TR-FRET assay[1].
VWK147 (10 μM; 3 h) does not bind to the HSP90 NTD in a fluorescence polarization assay[1].
VWK147 (25-100 μM; 1 h) inhibits HSP90 chaperone function in a cell-free luciferase refolding assay[1].
VWK147 (2-50 μM; 1 h) reduces HSP90α CTD dimers in a BS3 crosslinker assay[1].
VWK147 (1-10 μM; 6 h) destabilizes HSP90 client proteins ULK1, RIPK1, and CDK4 in Cisplatin-sensitive T24 and Cisplatin-resistant T24-CR urothelial carcinoma cells[1].
VWK147 (0.1-100 μM; 72 h) reduces cell viability in Cisplatin-sensitive (253J, T24) and -resistant (253J-CR, T24-CR) urothelial carcinoma cells with IC50 values of ~3-5 μM after 72 h[1].
VWK147 (10 μM; 0-24 h) induces cell death with both apoptotic and necrotic properties in T24 and T24-CR urothelial carcinoma cells over 24 h[1].
VWK147 (5 μM; 24 h) induced cell death in 253J, 253J-CR, T24, and T24-CR urothelial carcinoma cells is partially caspase-dependent[1].
VWK147 (1-10 μM; 6 h) induces concentration-dependent PARP1 cleavage in T24 and T24-CR urothelial carcinoma cells[1].
VWK147 (5 μM; 1-24 h) induces time-dependent PARP1 cleavage in T24 and T24-CR urothelial carcinoma cells over 24 h[1].
VWK147 (5 μM; 0-24 h) induces caspase-3 activation in Cisplatin-sensitive (253J, T24) and -resistant (253J-CR, T24-CR) urothelial carcinoma cells over 24 h[1].
VWK147 (5 μM; 6 h) inhibits autophagic flux in T24 and T24-CR urothelial carcinoma cells, as shown by LC3-II accumulation[1].
VWK147 (5 μM; 4 h) inhibits autophagosome-lysosome fusion in T24 and T24-CR urothelial carcinoma cells stably expressing mRFP-EGFP-rLC3[1].

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

VWK147 Related Antibodies

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.
Molecular Weight

674.71

Formula

C32H38N10O7
SMILES

CCC(N1C(C(NC(C2=NC=C(C(N2CC3=CC=C(C=C3)OC)=O)N)=O)=CN=C1C(NC4=CN=C(N(C4=O)CC(C)C)C(NC)=O)=O)=O)C
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Room temperature in continental US; may vary elsewhere.
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VWK147 Related Classifications

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Help & FAQs
  • 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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