ZXH-4-130 TFA是一种高效、选择性的CRBN降解剂，能够调节底物识别特性。
Cas No.:2711006-67-4
Sample solution is provided at 25 µL, 10mM.
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ZXH-4-130 TFA is an efficient and selective CRBN degrader, which can regulate substrate recognition characteristics [1]. ZXH-4-130 TFA restores the levels of GSPT1 proteins and prevent CDK9 degradation by degrading the CRBN protein [2]. ZXH-4-130 TFA is widely used as an alternative chemical probe for CRBN knockdown and as a model compound for site modification to develop novel molecules with high efficiency for targeting CRBN[3].
In vitro, ZXH-4-130 TFA treatment (100nM) for 2 hours significantly inhibited the cytotoxicity of pomalidomide against MM1.S cells and restored cell viability[4].
References:
[1] Fan G, Chen S, Zhang Q, et al. Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions[J]. MedComm, 2025, 6(10): e70401.
[2] Diehl C J, Ciulli A. Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders[J]. Chemical Society Reviews, 2022, 51(19): 8216-8257.
[3] Pichlak M, Sobierajski T, Błażewska K M, et al. Targeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues[J]. Journal of Enzyme Inhibition and Medicinal Chemistry, 2023, 38(1): 2254012.
[4] Powell C E, Du G, Bushman J W, et al. Selective degradation-inducing probes for studying cereblon (CRBN) biology[J]. RSC Medicinal Chemistry, 2021, 12(8): 1381-1390.
ZXH-4-130 TFA是一种高效、选择性的CRBN降解剂，能够调节底物识别特性[1]。ZXH-4-130 TFA通过降解CRBN蛋白，恢复GSPT1蛋白水平并阻止CDK9降解[2]。ZXH-4-130 TFA被广泛用作CRBN敲低的替代化学探针，并作为位点修饰的模型化合物，以开发高效靶向CRBN的新型分子[3]。
在体外，100nM的ZXH-4-130 TFA处理MM1.S细胞2小时，显著抑制了pomalidomide对MM1.S细胞的细胞毒性，并恢复了细胞活力[4]。
| Cell experiment [1]: | |
Cell lines | MM1.S cells |
Preparation Method | MM1.S cells were cultured at 37°C and 5% CO2 in RPMI-1640 media containing l-glutamine and 10% fetal bovine serum (FBS), 1% penicillin-streptomycin. Cells were plated at a density of 1×104 cells/ml in a 96-well plate with growth medium for 24h. MM1.S cell viability after 2h pre-treatments with 100nM of ZXH-4-130 TFA, ZXH-4-137, St-15a, or CRBN-6-5-5-VHL followed by 96-hour treatment with 1μM of pomalidomide. |
Reaction Conditions | 100nM; 2h |
Applications | ZXH-4-130 TFA treatment significantly inhibited the pomalidomide cytotoxicity and restored cell viability in MM1.S cells. |
References: | |
| Cas No. | 2711006-67-4 | SDF | Download SDF |
| 分子式 | C48H59F3N6O11S | 分子量 | 985.08 |
| 溶解度 | DMSO : 170 mg/mL (172.57 mM; Need ultrasonic) | 储存条件 | Store at -20°C, sealed storage, away from moisture and light |
| 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 | 1.0151 mL | 5.0757 mL | 10.1515 mL |
| 5 mM | 203 μL | 1.0151 mL | 2.0303 mL |
| 10 mM | 101.5 μL | 507.6 μL | 1.0151 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
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- Purity: >99.50% Appearance: A solid
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