VH 298
Modify Date: 2025-09-05 06:49:31
VH 298 structure
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Common Name | VH 298 | ||
|---|---|---|---|---|
| CAS Number | 2097381-85-4 | Molecular Weight | 523.65 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C27H33N5O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of VH 298VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology. |
| Name | VH-298 |
|---|
| Description | VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology. |
|---|---|
| Related Catalog | |
| Target |
Kd: 80 to 90 nM (VHL:HIF-α)[1] |
| In Vitro | VH-298 is a potent, cell permeable and non-toxic chemical probe that triggers the hypoxic response by blocking the VHL. VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with Kd values of 90 and 80 nM in isothermal titration calorimetry and competitive fluorescence polarization assay. VH-298 binds with VHL complex very fast and dissociates slowly. VH-298 at 50 μM concentration exhibits negligible off-target effects in vitro against more than 100 tested cellular kinases, GPCRs and ion channels. VH-298 is cell permeable and not toxic to cells. The measured permeability of VH-298 is found to be 19.4 nm s -1. VH-298 induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines, including HeLa cancer cells and renal cell carcinoma 4 (RCC4) cells. VH-298 increases mRNA levels of EPO by 2.5-fold in RCC4-HA-VHL, but not in VHL-null RCC4-HA, indicating that pharmacological inhibition of VHL is able to stimulate endogenous EPO synthesis. VH-298 proves as effective as hypoxia in raising PHD2 and HK2 protein levels, however in HFF the BNIP3 protein level increases more with VH-298 treatment than hypoxia treatment[1]. |
| Kinase Assay | VH-298 is screened at 50 μM concentration against a panel of 50 kinases. The remaining kinase activity is recorded in the end of the assay. The data is reported as average % activity remaining of assay duplicates for each kinase tested[1]. |
| Cell Assay | Death of CTLs is analyzed by staining with 4′,6-diamidino-2-phenylindole (DAPI). Cells are plated in 96-well plates at 1×106 and treated with VHL inhibitors (VH-298) and respective non-binding cis-analogues for 24 h. Cells are spun down and resuspended in HBSS containing DAPI to identify dead and dying populations[1]. |
| References |
| Molecular Formula | C27H33N5O4S |
|---|---|
| Molecular Weight | 523.65 |
| InChIKey | NDVQUNZCNAMROD-RZUBCFFCSA-N |
| SMILES | Cc1ncsc1-c1ccc(CNC(=O)C2CC(O)CN2C(=O)C(NC(=O)C2(C#N)CC2)C(C)(C)C)cc1 |
| Storage condition | 2-8℃ |
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