IKK2-IN-4
Based on 1 Customer Validation
IKK2-IN-4 is an orally active and selective IKK-2 inhibitor (IC50 = 0.025 μM) that also inhibits JNK-1 (IC50 = 1.6 μM). IKK2-IN-4 blocks IκB phosphorylation and NF-κB activation, and inhibits JNK-1 kinase activity. IKK2-IN-4 inhibits TNF-α production in PBMCs. IKK2-IN-4 can be used for research on IKK-2-related diseases, such as autoimmune diseases.
For research use only. We do not sell to patients.
- Purity : 98.51%
- CAS No.: 354811-10-2
- Formula: C12H11N3O2S
- Molecular Weight:261.30
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
IKK-2 0.025 μM (IC50) |
JNK1 1.6 μM (IC50) |
NF-κB |
TNF-α |
In Vitro
IKK2-IN-4 inhibits TNF-α production in PBMCs with a TNF cell IC50 of 0.25 μM; the WST-1 toxicity IC50 in PBMCs is 10 μM; Caco2 permeability is 17.7[1].
IKK2‑IN‑4 exhibits a clearance rate of 3 μL/min/106 cells in rat hepatocytes and a clearance rate of 27 μL/min/mg in human liver microsomes[1].
IKK2-IN-4 inhibits JNK-1 with an IC50 of 1.6 μM[1].
IKK2‑IN‑4 in complex with human JNK‑1 yields an X‑ray crystal structure at 2.1 Å resolution, which validates the modelled binding mode of IKK‑2, and all predicted hydrogen bonds are observed in the X‑ray structure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 354811-10-2
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Appearance Solid
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Molecular Weight 261.30
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Formula C12H11N3O2S
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Color Off-white to pink
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SMILES
O=C(C1=C(NC(N)=O)SC(C2=CC=CC=C2)=C1)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (382.70 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 (protect from light). 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 (protect from light). 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 (289 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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 (protect from light). 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 | 3.8270 mL | 19.1351 mL | 38.2702 mL | 95.6755 mL |
| 5 mM | 0.7654 mL | 3.8270 mL | 7.6540 mL | 19.1351 mL | |
| 10 mM | 0.3827 mL | 1.9135 mL | 3.8270 mL | 9.5675 mL | |
| 15 mM | 0.2551 mL | 1.2757 mL | 2.5513 mL | 6.3784 mL | |
| 20 mM | 0.1914 mL | 0.9568 mL | 1.9135 mL | 4.7838 mL | |
| 25 mM | 0.1531 mL | 0.7654 mL | 1.5308 mL | 3.8270 mL | |
| 30 mM | 0.1276 mL | 0.6378 mL | 1.2757 mL | 3.1892 mL | |
| 40 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3919 mL | |
| 50 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9135 mL | |
| 60 mM | 0.0638 mL | 0.3189 mL | 0.6378 mL | 1.5946 mL | |
| 80 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1959 mL | |
| 100 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL |
IKK2-IN-4 Related Classifications
HY-112456 Related Classifications
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