XIAP degrader-1
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.11%
- CAS No.: 2803617-91-4
- Formula: C34H45N5O4
- Molecular Weight:587.75
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) XIAP degrader-1
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Biological Activity
Description
IC50 & Target
[1]|
XIAP 1 μM (Kd) |
In Vitro
XIAP degrader-1 (compound 10) (0.01-10 μM; 8-16 h) potently reduces XIAP protein levels in MCF7 cells, with 98% degradation at 1 μM after 16 h, via a mechanism dependent on binding to XIAP but independent of cIAP[2].
XIAP degrader-1 (0.01-10 μM; 16 h) has a primary amine that is critical for its degradation activity, as modifications to this group that block ubiquitylation eliminate its ability to reduce XIAP protein levels in MCF7 cells[2].
XIAP degrader-1 (0.01-10 μM; 16 h) reduces wild-type HA-XIAP levels in transfected 293T cells, but does not degrade the RING-deficient HA-XIAPH467A mutant, demonstrating dependence on XIAP ligase function[2].
XIAP degrader-1 (1 μM; 0-16 h) undergoes XIAP-dependent ubiquitylation in a recombinant in vitro system, with formation of monoubiquitylated and polyubiquitylated species that is blocked by excess XIAP antagonist[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 human breast cancer cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:16 h, 8 h
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Result:Reduced XIAP levels to 2% of DMSO control levels after 16 h incubation with 1 μM reagent.
Induced maximal XIAP loss after 8 h incubation with 1 μM reagent.
Had its XIAP degradation effect blocked when co-incubated with 0.1 μM reagent and excess XIAP antagonist 1.
Maintained its XIAP degradation effect after pretreatment with 1 μM BV6.
Chemical Information
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CAS No. 2803617-91-4
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Appearance Solid
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Molecular Weight 587.75
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Formula C34H45N5O4
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Color Off-white to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Jun 26;15(1):5409. PMID: 38926334
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (170.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (287 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7014 mL | 8.5070 mL | 17.0140 mL | 42.5351 mL |
| 5 mM | 0.3403 mL | 1.7014 mL | 3.4028 mL | 8.5070 mL | |
| 10 mM | 0.1701 mL | 0.8507 mL | 1.7014 mL | 4.2535 mL | |
| 15 mM | 0.1134 mL | 0.5671 mL | 1.1343 mL | 2.8357 mL | |
| 20 mM | 0.0851 mL | 0.4254 mL | 0.8507 mL | 2.1268 mL | |
| 25 mM | 0.0681 mL | 0.3403 mL | 0.6806 mL | 1.7014 mL | |
| 30 mM | 0.0567 mL | 0.2836 mL | 0.5671 mL | 1.4178 mL | |
| 40 mM | 0.0425 mL | 0.2127 mL | 0.4254 mL | 1.0634 mL | |
| 50 mM | 0.0340 mL | 0.1701 mL | 0.3403 mL | 0.8507 mL | |
| 60 mM | 0.0284 mL | 0.1418 mL | 0.2836 mL | 0.7089 mL | |
| 80 mM | 0.0213 mL | 0.1063 mL | 0.2127 mL | 0.5317 mL | |
| 100 mM | 0.0170 mL | 0.0851 mL | 0.1701 mL | 0.4254 mL |
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