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VHL Ligand 1 hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VHL Ligand 1 is potential useful for the targeted degradation of the androgen receptor. VHL ligand 1 hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
| Molecular Weight | 467.02 |
| Formula | C22H31ClN4O3S |
| CAS Number | 1448189-80-7 |
| Solubility (25°C) | Water ≥ 50 mg/mL DMSO ≥ 30 mg/mL |
| Storage | -20°C, dry, sealed, protect from light |
| Related Ligand for E3 Ligase Products |
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| Pomalidomide
Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors. Pomalidomide is a second generation immunomodulator, TNF-α inhibitor with IC50 of 13 nM. |
| Thalidomide
Thalidomide is a sedative and immunomodulator used to study the symptoms of many cancers, it has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM. |
| VH-298
VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM. |
| E3 ligase Ligand 1
E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| E3 ligase Ligand 2
E3 ligase Ligand 2 (Thalidomide-4-OH) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can be connected to the ligand for protein by a linker to form PROTACs. |
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Products are for research use only. Not for human use. We do not sell to patients.
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