NI-42
目录号 : GC36734
An inhibitor of the BRPF1 bromodomain
Cas No.:1884640-99-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NI-42 is an inhibitor of the bromodomain and PHD finger-containing 1 (BRPF1) bromodomain (IC50 = 7.9 nM).1 It is selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively).2 NI-42 inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 acute myeloid leukemia (AML) cells (GI50s = 1.3, 4.6, 5.7, 7, and 9.9 ?M, respectively) and a variety of non-AML cells (GI50s = 1-10 ?M).1 It also inhibits the growth of DMS114 lung, HRA-19 colon, and RERF-LC-Sq1 lung cancer cells (GI50s = 16.6, 15.6, and 17.1 ?M, respectively) but not NCI H1703 lung cancer cells (GI50 = >30 ?M).2
1.Igoe, N., Bayle, E.D., Fedorov, O., et al.Design of a biased potent small molecule inhibitor of the bromodomain and PHD finger-containing (BRPF) proteins suitable for cellular and in vivo studiesJ. Med. Chem.60(2)668-680(2017) 2.Igoe, N., Bayle, E.D., Tallant, C., et al.Design of a chemical probe for the bromodomain and plant homeodomain finger-containing (BRPF) family of proteinsJ. Med. Chem.60(16)6998-7011(2017)
| Cas No. | 1884640-99-6 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(C#N)C=C1)(NC2=CC=C(N(C)C(C(C)=C3)=O)C3=C2)=O | ||
| 分子式 | C18H15N3O3S | 分子量 | 353.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | 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 | 2.8297 mL | 14.1483 mL | 28.2965 mL |
| 5 mM | 0.5659 mL | 2.8297 mL | 5.6593 mL |
| 10 mM | 0.283 mL | 1.4148 mL | 2.8297 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。
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies
J Med Chem 2017 Jan 26;60(2):668-680.PMID:28068087DOI:10.1021/acs.jmedchem.6b01583.
The BRPF (bromodomain and PHD finger-containing) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Evaluation of the BRPF family as a potential drug target is at an early stage although there is an emerging understanding of a role in acute myeloid leukemia (AML). We report the optimization of fragment hit 5b to 13-d as a biased, potent inhibitor of the BRD of the BRPFs with excellent selectivity over nonclass IV BRD proteins. Evaluation of 13-d in a panel of cancer cell lines showed a selective inhibition of proliferation of a subset of AML lines. Pharmacokinetic studies established that 13-d had properties compatible with oral dosing in mouse models of disease (Fpo 49%). We propose that NI-42 (13-d) is a new chemical probe for the BRPFs suitable for cellular and in vivo studies to explore the fundamental biology of these proteins.