NVS-ZP7-4
目录号 : GC34323
A ZIP7 inhibitor
Cas No.:2349367-89-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NVS-ZP7-4 is an inhibitor of the zinc transporter SLC39A7 (ZIP7).1 It induces apoptosis in TALL-1 human T cell acute lymphoblastic leukemia cells, an effect that can be reduced by expression of the ZIP7 point mutant ZIP7V430E. NVS-ZP7-4 (20 ?M) increases endoplasmic reticulum, but not cytosolic, zinc levels in U2OS cells. It inhibits ferroptosis induced by erastin in MDA-MB-231 and RCC4 cells when used at a concentration of 10 ?M.2
1.Nolin, E., Gans, S., Llamas, L., et al.Discovery of a ZIP7 inhibitor from a Notch pathway screenNat. Chem. Biol.15(2)179-188(2019) 2.Chen, P.-H., Wu, J., Xu, Y., et al.Zinc transporter ZIP7 is a novel determinant of ferroptosisCell Death Dis.12(2)198(2021)
| Cas No. | 2349367-89-9 | SDF | |
| Canonical SMILES | O=C(NC12CCN(C[C@@H](NC3=NC4=CC=C(F)C=C4S3)CC5=CC=CC=C5)CC2)NC6=C1C=CC=C6 | ||
| 分子式 | C28H28FN5OS | 分子量 | 501.62 |
| 溶解度 | DMSO : ≥ 125 mg/mL (249.19 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | -20°C, protect from 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 | 1.9935 mL | 9.9677 mL | 19.9354 mL |
| 5 mM | 0.3987 mL | 1.9935 mL | 3.9871 mL |
| 10 mM | 0.1994 mL | 0.9968 mL | 1.9935 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。
Discovery of a ZIP7 inhibitor from a Notch pathway screen
Nat Chem Biol 2019 Feb;15(2):179-188.PMID:30643281DOI:PMC7251565
The identification of activating mutations in NOTCH1 in 50% of T cell acute lymphoblastic leukemia has generated interest in elucidating how these mutations contribute to oncogenic transformation and in targeting the pathway. A phenotypic screen identified compounds that interfere with trafficking of Notch and induce apoptosis via an endoplasmic reticulum (ER) stress mechanism. Target identification approaches revealed a role for SLC39A7 (ZIP7), a zinc transport family member, in governing Notch trafficking and signaling. Generation and sequencing of a compound-resistant cell line identified a V430E mutation in ZIP7 that confers transferable resistance to the compound NVS-ZP7-4. NVS-ZP7-4 altered zinc in the ER, and an analog of the compound photoaffinity labeled ZIP7 in cells, suggesting a direct interaction between the compound and ZIP7. NVS-ZP7-4 is the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.