VH298
Description In vitro In vivo- Product Name
- VH298
- CAS No.
- 2097381-85-4
- Chemical Name
- VH298
- Synonyms
- VH298;VHL-298;CS-2647;VH298;VH 298;VH298 USP/EP/BP;E3 ligase-recruiting Moiety,VH-298,Inhibitor,VH298,Ligands for E3 Ligase,VH 298,inhibit;L-Prolinamide, N-[(1-cyanocyclopropyl)carbonyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;(2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-((S)-2-(1-Cyanocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-[(1-cyanocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
- CBNumber
- CB73344894
- Molecular Formula
- C27H33N5O4S
- Formula Weight
- 523.65
- MOL File
- 2097381-85-4.mol
VH298 Property
- Boiling point:
- 860.8±65.0 °C(Predicted)
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMF:30.0(Max Conc. mg/mL);57.29(Max Conc. mM)
DMSO:66.42(Max Conc. mg/mL);126.84(Max Conc. mM)
Ethanol:60.79(Max Conc. mg/mL);116.09(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:9):0.1(Max Conc. mg/mL);0.19(Max Conc. mM) - form
- A crystalline solid
- pka
- 12.28±0.20(Predicted)
- color
- Off-white to pink
- InChIKey
- NDVQUNZCNAMROD-RZUBCFFCSA-N
- SMILES
- C(NCC1=CC=C(C2SC=NC=2C)C=C1)(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@H](C(C)(C)C)NC(C1(C#N)CC1)=O
N-Bromosuccinimide Price
- Product number
- 21133
- Product name
- VH298
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 21133
- Product name
- VH298
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $98
- Updated
- 2024/03/01
- Product number
- 21133
- Product name
- VH298
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $178
- Updated
- 2024/03/01
- Product number
- 21133
- Product name
- VH298
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $397
- Updated
- 2024/03/01
- Product number
- 6156
- Product name
- VH298
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $244
- Updated
- 2021/12/16
VH298 Chemical Properties,Usage,Production
Description
VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology.
In vitro
VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.
In vivo
VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.
Description
VH-298 is a E3 ligase ligand-linker conjugate that couples the VHL ligand and blocks the interaction between VHL and HIF-α, initiating hypoxic response.
Uses
(2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide is a VHL inhibitors that decreases hypoxia inducible factor-α during hypoxia associated signaling in human cervical cancer, osteosarcoma HeLa and U2OS. cells.
Biological Activity
HIF-1α and hydroxy-HIF-1α levels increased in VH298-treated rFb in a time- and dose-dependent manner. Thirty micromolar VH298 could significantly increase cell proliferation, angiogenesis, and gene expression of type I collagen-α1 (Col1-α1), vascular endothelial growth factor A (VEGF-A), and insulin-like growth factor 1 (IGF-1). The VH298-treated wound had a better healing pattern, activation of HIF-1 signaling, and vascularization. It is is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechan: the the blockade of the VHL: HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes. It engages with high affinity and specificity with VHL as its only primary cellular target, leading to selective on-target accumulation of hydroxylated HIF-α in a concentration- and time-dependent fashion in different cell lines, with subsequent upregulation of HIF-target genes at both mRNA and protein levels[1-2].
storage
Store at -20°C
References
[1] Julianty Frost. “Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition.” Nature Communications 7 1 (2016).
[2] Shuo Qiu. “Von Hippel-Lindau (VHL) Protein Antagonist VH298 Improves Wound Healing in Streptozotocin-Induced Hyperglycaemic Rats by Activating Hypoxia-Inducible Factor- (HIF-) 1 Signalling.” Journal of Diabetes Research (2019): 1897174.
VH298 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from VH298 manufacturers
- Product
- VH-298 2097381-85-4
- Price
- US $0.00-0.00/MG
- Min. Order
- 1MG
- Purity
- 98%+ HPLC HNMR
- Supply Ability
- 50 g per month
- Release date
- 2024-03-29
- Product
- VH298 2097381-85-4
- Price
- US $1.00/kg
- Min. Order
- 1kg
- Purity
- 95%-99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24