SB-405483
Based on 1 Customer Validation
SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.33%
- 화학식: C20H16N4O3
- 분자량:360.37
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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CK1α |
IKZF1 |
IKZF3 |
SB-405483 (2.5-25 μM) binds the recombinant human CRBN/DDB1 complex with a binding potency of 25 ± 0.9 μM and exhibits highly synergistic binding with the lenalidomide-Alexa647 probe[1].
SB-405483 (25 μM) potentiates the binding of multiple orthosteric CRBN ligands to the recombinant human CRBN/DDB1 complex, as shown by 8.96- to 43.7-fold decreases in their IC50 values, with no effect on mezigdomide binding[1].
SB-405483 (0.1-25 μM; 1 h) stabilizes endogenous CRBN in MM.1S cells in a dose-dependent manner, with enhanced stabilization when co-treated with Lenalidomide (HY-A0003)[1].
SB-405483 (0.1-10 μM) inhibits autoubiquitination of endogenous Flag-tagged CRBN in HEK293T cells in a dose-dependent manner[1].
SB-405483 (10 μM; 0.5-24 h) potentiates DEG-47-mediated degradation of endogenous CK1α in MOLM-13 cells[1].
SB-405483 (10 μM; 24 h) potentiates DEG-47-mediated degradation of Wee1 in A2780 Wee1-HiBiT cells and MOLM-13 cells[1].
SB-405483 (10 μM; 24 h) inhibits DEG-47-mediated degradation of IKZF1/3(ZF2)-GFP and IKZF2(ZF2)-GFP in HEK293T reporter cells after 24 h[1].
SB-405483 (10 μM; 24 h) modestly potentiates DEG-47-mediated degradation of SALL4(ZF1,2)-GFP in U937 Cas9 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human acute myeloid leukemia MOLM-13 cells
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Concentration:10 μM
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Incubation Time:0.5, 1, 2, 4, 6, 24 h
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Result:Decreased the DC50 of DEG-47 from 21 nM to 5 nM in a GFP-CK1α reporter assay after 24 h.
Reduced CK1α expression.
Chemical Information
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Appearance Solid
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분자량 360.37
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화학식 C20H16N4O3
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Color White to light brown
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SMILES
O=C(NC1=CC=C(C#N)C=C1O)NC2=NC=CC=C2OCC3=CC=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
DMSO : 25 mg/mL (69.37 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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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)
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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 (stored under nitrogen). 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 | 2.7749 mL | 13.8746 mL | 27.7493 mL | 69.3731 mL |
| 5 mM | 0.5550 mL | 2.7749 mL | 5.5499 mL | 13.8746 mL | |
| 10 mM | 0.2775 mL | 1.3875 mL | 2.7749 mL | 6.9373 mL | |
| 15 mM | 0.1850 mL | 0.9250 mL | 1.8500 mL | 4.6249 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3875 mL | 3.4687 mL | |
| 25 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7749 mL | |
| 30 mM | 0.0925 mL | 0.4625 mL | 0.9250 mL | 2.3124 mL | |
| 40 mM | 0.0694 mL | 0.3469 mL | 0.6937 mL | 1.7343 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL |
SB-405483 Related Classifications
HY-W1135319 Related Classifications
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