SP3N hydrochloride
Based on 1 Customer Validation
SP3N hydrochloride is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N hydrochloride is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N hydrochloride induces the proximity of FKBP12 to the SCFFBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N hydrochloride can be used in cancer research.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.84%
- 화학식: C39H58ClN3O10
- 분자량:764.34
-
보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
IC50 & Target
|
FKBP12 |
In Vitro
SP3N (1 nM-10 μM; 1-16 h) hydrochloride potently degrades FKBP12 in KBM7 iCas9 FKBP12-BFP-P2A-mCherry reporter cells in a time- and dose-dependent manner, and this degradation depends on the ubiquitin-proteasome system and Cullin-RING ligase activity[1].
SP3N (1 μM; 16 h) hydrochloride degrades FKBP12 in HEK293T cells, with no detectable off-target degradation across the proteome after 16 h of 1 μM treatment[1].
SP3N (0.001-20 μM; 16 h) hydrochloride dose-dependently reduces FKBP12 protein levels in HEK293T Nluc-3xFlag-FKBP12-NLS cells after 16 h of treatment[1].
SP3N hydrochloride requires metabolic conversion by amine oxidases (such as DAO) to an active species to induce FKBP12 degradation in KBM7 iCas9 FKBP12-BFP-P2A-mCherry reporter cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T Nluc-3xFlag-FKBP12-NLS cells
-
Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM
-
Incubation Time:16 h
-
Result:Reduced FKBP12 protein levels in a dose-dependent manner.
Started detectable degradation at 0.01 μM.
Achieved near-complete degradation at 20 μM.
Chemical Information
-
Appearance Solid
-
분자량 764.34
-
화학식 C39H58ClN3O10
-
Color Colorless to off-white
-
SMILES
COC1=CC=C(CC[C@@H](OC([C@@H]2CCCCN2C(C(C(C)(C)CC)=O)=O)=O)C3=CC(NC(CCOCCOCCOCCN)=O)=CC=C3)C=C1OC.Cl
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
DMSO : 100 mg/mL (130.83 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
순도&문서
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3083 mL | 6.5416 mL | 13.0832 mL | 32.7080 mL |
| 5 mM | 0.2617 mL | 1.3083 mL | 2.6166 mL | 6.5416 mL | |
| 10 mM | 0.1308 mL | 0.6542 mL | 1.3083 mL | 3.2708 mL | |
| 15 mM | 0.0872 mL | 0.4361 mL | 0.8722 mL | 2.1805 mL | |
| 20 mM | 0.0654 mL | 0.3271 mL | 0.6542 mL | 1.6354 mL | |
| 25 mM | 0.0523 mL | 0.2617 mL | 0.5233 mL | 1.3083 mL | |
| 30 mM | 0.0436 mL | 0.2181 mL | 0.4361 mL | 1.0903 mL | |
| 40 mM | 0.0327 mL | 0.1635 mL | 0.3271 mL | 0.8177 mL | |
| 50 mM | 0.0262 mL | 0.1308 mL | 0.2617 mL | 0.6542 mL | |
| 60 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5451 mL | |
| 80 mM | 0.0164 mL | 0.0818 mL | 0.1635 mL | 0.4088 mL | |
| 100 mM | 0.0131 mL | 0.0654 mL | 0.1308 mL | 0.3271 mL |
SP3N hydrochloride Related Classifications
HY-161794A Related Classifications
Powered by Bioz