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PROTAK™ Gefitinib-based PROTAC 3
$280/ 1mg
Specification
QuantityTotal: $280
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Product Information
CAS No.2230821-27-7
Purity>98.00%
FormulaC27H33N5O4S
M.W.934.522
SolubilitySoluble in DMSO
Storage/StabilityStore at -20°C
BackgroundVH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.VH-298 is a potent, cell permeable and non-toxic chemical probe that triggers the hypoxic response by blocking the VHL. VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with Kd values of 90 and 80 nM in isothermal titration calorimetry and competitive fluorescence polarization assay. VH-298 binds with VHL complex very fast and dissociates slowly. VH-298 at 50 uM concentration exhibits negligible off-target effects in vitro against more than 100 tested cellular kinases, GPCRs and ion channels. VH-298 is cell permeable and not toxic to cells. The measured permeability of VH-298 is found to be 19.4 nm s -1. VH-298 induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines, including HeLa cancer cells and renal cell carcinoma 4 (RCC4) cells. VH-298 increases mRNA levels of EPO by 2.5-fold in RCC4-HA-VHL, but not in VHL-null RCC4-HA, indicating that pharmacological inhibition of VHL is able to stimulate endogenous EPO synthesis. VH-298 proves as effective as hypoxia in raising PHD2 and HK2 protein levels, however in HFF the BNIP3 protein level increases more with VH-298 treatment than hypoxia treatment
PROTAK™ is a registered trademark of EnoGene.
PROTAK™ is a registered trademark of EnoGene.
Price280$
Number: E31P19509-1, E31P19509-2 Name: PROTAK™ Gefitinib-based PROTAC 3
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