BC-1471是一种STAMBP去泛素化酶抑制剂，IC50值为0.33µM。
Cas No.:896683-84-4
Sample solution is provided at 25 µL, 10mM.
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BC-1471 is a STAMBP deubiquitinase inhibitor with an IC50 of 0.33μM [1]. BC-1471 can inhibit the cleavage of di-ubiquitin and block the ability of recombinant STAMBP to deubiquitinate the physiologically relevant substrate Ub-NALP7 [2]. BC-1471 has been widely used for regulating deubiquitination processes, and has also been employed as a model compound to screen specific STAMBP inhibitors[3].
In vitro, BC-1471 pretreatment for 2h at 10μM resulted in a significant decrease in the endogenous NALP7 abundance in THP-1 cells[4]. BC-1471 pretreatment (10μM) for 2 hours inhibited the release of IL-1β in human peripheral blood mononuclear cells (PBMCs) exposed to lipopolysaccharide (LPS)[4].
References:
[1] Pan X, Wu S, Wei W, et al. Structural and functional basis of JAMM deubiquitinating enzymes in disease[J]. Biomolecules, 2022, 12(7): 910.
[2] Schauer N J, Magin R S, Liu X, et al. Advances in discovering deubiquitinating enzyme (DUB) inhibitors[J]. Journal of medicinal chemistry, 2019, 63(6): 2731-2750.
[3] Wu H Q, Baker D, Ovaa H. Small molecules that target the ubiquitin system[J]. Biochemical Society Transactions, 2020, 48(2): 479-497.
[4] Bednash J S, Weathington N, Londino J, et al. Targeting the deubiquitinase STAMBP inhibits NALP7 inflammasome activity[J]. Nature communications, 2017, 8(1): 15203.
BC-1471是一种STAMBP去泛素化酶抑制剂，IC50值为0.33µM[1]。BC-1471 能够抑制二聚化的泛素的裂解过程，并阻断重组的STAMBP对生理相关底物 Ub-NALP7 的去泛素化能力[2]。BC-1471已被广泛用于调控去泛素化过程，并作为模型化合物用于筛选特异性STAMBP抑制剂[3]。
在体外，使用10µM的BC-1471预处理THP-1细胞2小时，导致内源性NALP7丰度显著下降[4]。用10µM的BC-1471预处理2小时，抑制了暴露于脂多糖（LPS）的人外周血单核细胞（PBMCs）中IL-1β的释放[4]。
| Cell experiment [1]: | |
Cell lines | THP-1 cells |
Preparation Method | THP-1 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). THP-1 cells (1×106 per ml) were pre-treated with BC-1471 (10μM) for 2h prior to addition of LPS (500ng) or control for 6h, and the level of pro-IL-1β mRNA was detected. |
Reaction Conditions | 10μM; 2h |
Applications | BC-1471 treatment enhanced the levels of pro-IL-1β mRNA in THP-1 cells exposed to LPS. |
References: | |
| Cas No. | 896683-84-4 | SDF | Download SDF |
| 分子式 | C27H32N4O4S | 分子量 | 508.63 |
| 溶解度 | DMSO : 50 mg/mL (98.30 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 | 1.9661 mL | 9.8303 mL | 19.6607 mL |
| 5 mM | 393.2 μL | 1.9661 mL | 3.9321 mL |
| 10 mM | 196.6 μL | 983 μL | 1.9661 mL |
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| 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 |
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| % 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。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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