3079093-92-5
Chemical Structure
TMX1
- CAS No.: 3079093-92-5
- Formula:C26H28N4O3S
- Molecular Weight:476.59
IUPAC Name: tert-butyl (S,E)-2-(2,3,9-trimethyl-4-(4-(3-oxoprop-1-en-1-yl)phenyl)-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
InChIKey: SJISOGWQGIVAGX-DUIUGDAFSA-N
SMILES: O=C/C=C/C1=CC=C(C2=N[C@@H](CC(OC(C)(C)C)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4)C=C1
Biological Activity: TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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TMX1 | 99.57% | TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity. | ||||||||||||||||||||
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- [1]. Li YD, et al. Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. bioRxiv [Preprint]. 2023 Feb 15:2023.02.14.528208. [Content Brief]
- [2]. Li YD, et al. Template-assisted covalent modification underlies activity of covalent molecular glues. Nat Chem Biol. 2024;20(12):1640-1649. [Content Brief]
Keywords
