[CAS NO. 1013753-99-5] BC-1382
PRODUCTS SPECIFICATIONS [1013753-99-5]
DESCRIPTION [1013753-99-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 459.56 |
| Molecular Formula | C23H29N3O5S |
| SMILES | O=C(C1CCN(S(=O)(C2=CC=CC=C2)=O)CC1)N[C@@H](C)C(NCC3=CC=CC=C3OC)=O |
Summary
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction ( IC 50 ≈ 5 nM).Anti-inflammatory activity [1] .
In Vitro
BC-1382 targets HECTD2 and attenuates lipopolysaccharide (LPS)– and Pseudomonas aeruginosa-induced lung inflammation. HECTD2 is an ubiquitin E3 ligase. BC-1382 reduces the severity of cytokine-driven lung inflammation
[1]
.
BC-1382 drastically increases PIAS1 protein level in a nonstimulus condition with IC
50
≈100 nM
[1]
.
BC-1382 improves PIAS1 protein stability by increasing its t1/2
[1]
.
BC-1382 suppresses LPS-induced PIAS1 degradation and restores PIAS1 protein levels at 800 nM
[1]
.
BC-1382 suppresses LPS-induced proinflammatory cytokines released by human peripheral blood mononuclear cells (PBMCs)
[1]
.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BC-1382 (10 mg/kg; intraperitoneal injection) significantly decreases lavage protein concentrations, lavage cell counts, and cell infiltrates in both PA103-stimulated and LPS-stimulated mice. BC-1382 significantly decreases lavage cytokine levels in both models [1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6J mice were challenged intratracheally with PA103 (104 CFU per mouse) or LPS (3 mg/kg) [1] |
| Dosage: | 10 mg/kg |
| Administration: | Given through intraperitoneal injection |
| Result: |
Significantly decreased lavage protein concentrations, lavage cell counts, and cell infiltrates in both PA103-stimulated and LPS-stimulated mice.
Significantly decreased lavage cytokine levels in both models. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 125 mg/mL ( 272.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1760 mL | 10.8800 mL | 21.7599 mL |
| 5 mM | 0.4352 mL | 2.1760 mL | 4.3520 mL |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1760 mL |
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