BC-1382
目录号 : GC68150BC-1382 是一种有效的泛素 E3 连接酶 HECTD2 抑制剂，可特异性破坏 HECTD2/PIAS1 相互作用 (IC50≈ 5 nM)。具有抗炎活性。
Cas No.:1013753-99-5
Sample solution is provided at 25 µL, 10mM.
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BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity[1].
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 IC50≈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].
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].
| 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. |
[1]. Tiffany A Coon, et al. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109.
| Cas No. | 1013753-99-5 | SDF | Download SDF |
| 分子式 | C23H29N3O5S | 分子量 | 459.56 |
| 溶解度 | DMSO : 125 mg/mL (272.00 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.176 mL | 10.88 mL | 21.7599 mL |
| 5 mM | 0.4352 mL | 2.176 mL | 4.352 mL |
| 10 mM | 0.2176 mL | 1.088 mL | 2.176 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet