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VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes. 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 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.
| Molecular Weight | 523.65 |
| Formula | C27H33N5O4S |
| CAS Number | 2097381-85-4 |
| Solubility (25°C) | DMSO: ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ligand for E3 Ligase Products |
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| OICR-8268
OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can be used in the development of DCAF1-based PROTACs. |
| BC-1215
BC-1215 is a novel inhibitor of F-box protein 3 (Fbxo3) activity. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 relieves allodynia by preventing ubiquitination-dependent Fbxl2/TRAF2/TNIK/pGluR1 signaling. BC-1215 exerted robust therapeutic effects in cytokine-driven inflammation, including pseudomona-induced lung injury and cecum ligation/punctured-induced sepsis, by targeting Fbxo3/Fbxl2/TRAF-mediated cytokine release. BC-1215 can be used for the research of inflammation. |
| VH 101, acid
VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. |
| (S,R,S)-AHPC-Boc
(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| Lenalidomide-Br
Lenalidomide-Br is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. |
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