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Product Information:

TMX1

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.

Cat. No.: EX-A11426    Purity: >98%
Chemical
Chemical structure of TMX1


For research only, Do not use for Human!

SizeUnit Price (US$)StockQuantityOrder
50mg1180Inquire
100mg1880Inquire
250mg3580Inquire
500mg5680Inquire


CAS No.3079093-92-5
Purity>98%
FormulaC26H28N4O3S
Mol Weight476.591
ColorWhite to off-white
StateSolid
SolubilityDMSO : ? 100 mg/mL
Shelf Life>3 years if stored properly
StoragePowder 4°C, sealed storage, away from moisture and light; In solvent -20℃ 1 month;
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  

[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.

[2]. Li YD, et al. Template-assisted covalent modification underlies activity of covalent molecular glues. Nat Chem Biol. 2024;20(12):1640-1649.

CoACoA of TMX1
Smiles:CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)/C=C/C=O)C

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