2. Metabolic Enzyme/Protease PROTAC
  3. HIF/HIF Prolyl-Hydroxylase Ligands for E3 Ligase E1/E2/E3 Enzyme
  4. VHL-IN-1

VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research.

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VHL-IN-1

VHL-IN-1 Chemical Structure

CAS No. : 3033117-53-9

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VHL-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

View All Isoforms
HIF-1α HIF

View All Ligands for E3 Ligase Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B KLHL41

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  • Purity & Documentation

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Description

VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research[1].

IC50 & Target[1]

VHL

37 nM (Kd)

HIF-1α

 

In Vitro

VHL-IN-1 potently binds to the VCB complex, with a dissociation constant of 37 nM as measured by fluorescence polarization (FP)[1].
VHL-IN-1 (1.37-1000 nM) binds strongly to the VCB complex, with a dissociation constant of 25 nM measured by SPR[1].
VHL-IN-1 (50 μM; 2 h) potently stabilizes total HIF-1α and hydroxylated HIF-1α in HeLa and HEK 293 cells. At the concentration of 50 μM, its induced total HIF-1α level reaches 182-224% of that induced by VH298, while the induced HIF-1α-OH level reaches 208-263% of that induced by VH298[1].
VHL-IN-1 (50-150 μM; 16 h) potently upregulates the mRNA expression of CA9 in HeLa cells, and its effects at concentrations of 100 μM and 150 μM are significantly superior to those of VH298[1].

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

VHL-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HeLa, HEK 293
Concentration: 50 μM
Incubation Time: 2 h
Result: Stabilized total HIF-1α to 182% of reference levels in HeLa cells and 224% in HEK 293 cells at 50 μM.
Stabilized HIF-1α-OH to 263% of reference levels in HeLa cells and 208% in HEK 293 cells at 50 μM.

Real Time qPCR[1]

Cell Line: HeLa
Concentration: 50-150 μM
Incubation Time: 16 h
Result: Significantly upregulated CA9 mRNA levels at 50 μM.
Greatly outperformed the reference inhibitor VH298 at 100 and 150 μM, reaching relative levels ~800-900% of the DMSO control at these concentrations.
Molecular Weight

544.68

Formula

C28H37FN4O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (183.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8359 mL 9.1797 mL 18.3594 mL
5 mM 0.3672 mL 1.8359 mL 3.6719 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8359 mL 9.1797 mL 18.3594 mL 45.8985 mL
5 mM 0.3672 mL 1.8359 mL 3.6719 mL 9.1797 mL
10 mM 0.1836 mL 0.9180 mL 1.8359 mL 4.5899 mL
15 mM 0.1224 mL 0.6120 mL 1.2240 mL 3.0599 mL
20 mM 0.0918 mL 0.4590 mL 0.9180 mL 2.2949 mL
25 mM 0.0734 mL 0.3672 mL 0.7344 mL 1.8359 mL
30 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5300 mL
40 mM 0.0459 mL 0.2295 mL 0.4590 mL 1.1475 mL
50 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9180 mL
60 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7650 mL
80 mM 0.0229 mL 0.1147 mL 0.2295 mL 0.5737 mL
100 mM 0.0184 mL 0.0918 mL 0.1836 mL 0.4590 mL
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VHL-IN-1 Related Classifications

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:

VHL-IN-13033117-53-9HIF/HIF Prolyl-HydroxylaseLigands for E3 LigaseE1/E2/E3 EnzymeHypoxia-inducible factorsHIFsHIF-PHE3 ligase-recruiting MoietyE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasehydroxylated HIF-1αvon Hippel-Lindau (VHL) E3 ubiquitin ligaseVCB complexCA9 mRNAHEK 293 cellshuman serum albuminHIF-1αTyr98HeLa cellshypoxia signaling pathwayInhibitorinhibitorinhibit

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