2409538-70-9
Chemical Structure
GAL-02-221
Synonym(s): PROTAC BRD4 Degrader-5
- CAS No.: 2409538-70-9
- Formula:C50H62ClN9O8S2
- Molecular Weight:1016.67
IUPAC Name: (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
InChIKey: SLPWRCRRHVRNRM-BEGQQDOQSA-N
SMILES: O=C([C@H]1N(C([C@H](C(C)(C)C)NC(COCCOCCOCCNC(C[C@H]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2)=O)=O)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
Biological Activity: GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC50 of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GAL-02-221 | 99.87% | GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC50 of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer. | ||||||||||||||||||||
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- [1]. Maneiro MA, et al. Antibody-PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4. ACS chemical biology. 2020 Jun 19;15(6):1306-1312. [Content Brief]
- [2]. Leconte GA, et al. A Lipid Prodrug Strategy Enhances Targeted Protein Degrader CNS Pharmacokinetics. Journal of medicinal chemistry. 2025 Aug 28;68(16):17339-17349. [Content Brief]
Keywords
