3034880-93-5
Chemical Structure
VVD-130037
Synonym(s): BAY-3605349
- CAS No.: 3034880-93-5
- Formula:C17H17ClN4O2
- Molecular Weight:344.80
InChIKey: IRLNMPCPLJZIGO-AWEZNQCLSA-N
SMILES: NC1=NC(C2=CC(Cl)=CC([C@@H]3COCCN3C(C=C)=O)=C2)=NC=C1
Biological Activity: VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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VVD-130037 | 99.91% | VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors. | ||||||||||||||||||||
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- [1]. Housand C, et al. Translational pharmacokinetic/pharmacodynamic (PK/PD) modeling for VVD-130037, a novel, first-in-class covalent small molecule Kelch-like ECH-associated protein 1 (KEAP1) activator[J]. Cancer Research, 2025, 85(8_Supplement_1): 4349-4349.
- [2]. Burston H E, et al. Mechanisms that matter: unbiased cellular screening for degraders[J]. npj Drug Discovery, 2025, 2(1): 26.
- [3]. Li Y, et al. Lymphatic Metastasis of Esophageal Squamous Cell Carcinoma: The Role of NRF2 and Therapeutic Strategies. Cancers (Basel). 2025;17(11):1853. Published 2025 May 31. [Content Brief]
- [4]. Han B, et al. Tumor suppressor KEAP1 promotes HSPA9 degradation, controlling mitochondrial biogenesis in breast cancer. Cell Rep. 2024;43(7):114507. [Content Brief]
Keywords
