2803617-91-4
Chemical Structure
XIAP degrader-1
- CAS No.: 2803617-91-4
- Formula:C34H45N5O4
- Molecular Weight:587.75
IUPAC Name: (S)-N-((2S,3S)-1-(8-aminooctanoyl)-5-((2-methoxynaphthalen-1-yl)methyl)-2-methyl-4-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)-2-(methylamino)propanamide
InChIKey: MCVQOARFDZLCRN-TWVHRYOLSA-N
SMILES: CN[C@H](C(N[C@@H]1C(N(C2=C(N([C@H]1C)C(CCCCCCCN)=O)C=CC=C2)CC3=C(C=CC=C4)C4=CC=C3OC)=O)=O)C
Biological Activity: XIAP degrader-1 is a PROTAC-like degrader with a Kd value of 1 μM for XIAP. XIAP degrader-1 is metabolized into an active aldehyde species that covalently binds to Cys326 of FBXO22, thereby forming a ternary complex with the BIR2 domain of XIAP. XIAP degrader-1 induces polyubiquitination and proteasomal degradation of XIAP via the ubiquitin-proteasome system, a process dependent on NEDD8 conjugation, the SCFFBXO22 ligase complex, as well as the functional activities of XIAP ligase, E1 and the proteasome[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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XIAP degrader-1 | 98.11% | XIAP degrader-1 is a PROTAC-like degrader with a Kd value of 1 μM for XIAP. XIAP degrader-1 is metabolized into an active aldehyde species that covalently binds to Cys326 of FBXO22, thereby forming a ternary complex with the BIR2 domain of XIAP. XIAP degrader-1 induces polyubiquitination and proteasomal degradation of XIAP via the ubiquitin-proteasome system, a process dependent on NEDD8 conjugation, the SCFFBXO22 ligase complex, as well as the functional activities of XIAP ligase, E1 and the proteasome. | ||||||||||||||||||||
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References
- [1]. Kagiou C, et al. Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation. Nature communications. 2024 Jun 26;15(1):5409. [Content Brief]
- [2]. den Besten W, et al. Primary Amine Tethered Small Molecules Promote the Degradation of X-Linked Inhibitor of Apoptosis Protein. Journal of the American Chemical Society. 2021 Jul 21;143(28):10571-10575. [Content Brief]
