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VH-298

產(chǎn)品活性：VH-298是高效的 VHL:HIF-α 相互作用抑制劑， K_d 值為80-90 nM。 VH-298可用于 PROTAC 技術(shù)中。

研究領(lǐng)域：PROTAC

作用靶點(diǎn)：Ligands for E3 Ligase

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 K_d 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.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Ubiquitination Compound Library  |  E3 Ligase Ligand Library  |  Heterocyclic Compound Library  |  Lenalidomide hydrochloride  |  Thalidomide-NH-CH2-COOH  |  Pomalidomide-d₃  |  Thalidomide-5-propoxyethanamine  |  Pomalidomide-5-O-CH3  |  BODIPY FL thalidomide  |  VH032-OH  |  TD-106  |  SJPYT-195  |  Lenalidomide-5-aminomethyl hydrochloride  |  BC-1215  |  Thalidomide-5-propargyne-NH2 hydrochloride  |  Thalidomide 5-fluoride  |  VH032 thiol  |  Lenalidomide-5-Br  |  CRBN modulator-1  |  E3 ligase Ligand 21  |  Pomalidomide-C5-Dovitinib  |  Lenalidomide-6-F  |  E3 ligase Ligand 8  |  LCL-PEG3-N3 hydrochloride  |  Thalidomide-5-PEG2-Cl  |  Golcadomide  |  Cemsidomide  |  Thalidomide-O-C8-COOH  |  CC-885  |  ALV2  |  Thalidomide-5-methyl  |  E3 ligase Ligand 13  |  Pomalidomide-C11-NH2

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