HMN-154
目录号 : GC33321
HMN-154是一种新型的苯磺酰胺类抗癌化合物。HMN-154与NF-YB相互作用，从而中断NF-Y异源三聚体与DNA的结合。
Cas No.:173528-92-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cells are seeded into a 96-well microplate at a cell density of 10000/well. Drug is added on the next day, and the plate then is incubated for 72 h at 37°C. The growth inhibitory concentration is measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay[1]. |
References: [1]. Tanaka H, et al. Isolation of cDNAs encoding cellular drug-binding proteins using a novel expression cloning procedure: drug-western. Mol Pharmacol. 1999 Feb;55(2):356-63. | |
HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.
HMN-154 interacts with NF-YB and thereby interrupts the binding of the NF-Y heterotrimer to DNA. NF-YB and thymosin β-10 are specific cellular binding proteins of HMN-154 and that this shared region is necessary for the binding to HMN-154. HMN-154 inhibits DNA binding of NF-Y to the human major histocompatibility complex class II human leukocyte antigen DRA Y-box sequence in a dose-dependent manner. HMN-154 shows very strong cytotoxicity against KB and colon38 cells with an IC50 value of 0.0026 and 0.003 μg/mL, respectively. HMN-154/BSA binds recombinant NF-YB or thymosin β-10 and the binding is inhibited by the addition of HMN-154 as the competitor. The binding between HMN-154 and NF-YB is specific and depends on its cytotoxicity[1].
[1]. Tanaka H, et al. Isolation of cDNAs encoding cellular drug-binding proteins using a novel expression cloning procedure: drug-western. Mol Pharmacol. 1999 Feb;55(2):356-63.
| Cas No. | 173528-92-2 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(OC)C=C1)(NC2=CC=CC=C2/C=C/C3=CC=NC=C3)=O | ||
| 分子式 | C20H18N2O3S | 分子量 | 366.43 |
| 溶解度 | DMSO : ≥ 15 mg/mL (40.94 mM) | 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 | 2.729 mL | 13.6452 mL | 27.2903 mL |
| 5 mM | 0.5458 mL | 2.729 mL | 5.4581 mL |
| 10 mM | 0.2729 mL | 1.3645 mL | 2.729 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。
Isolation of cDNAs encoding cellular drug-binding proteins using a novel expression cloning procedure: drug-western
Mol Pharmacol 1999 Feb;55(2):356-63.PMID:9927629DOI:10.1124/mol.55.2.356
A rapid and convenient new method for isolating the genes encoding cellular drug-binding proteins is described. This method, drug-western, is based on the use of the drug conjugated with a marker molecule as a probe for the screening of a cDNA library. Unlike the other methods, this method allows us to identify the genes for trace amounts of cellular drug-binding proteins without purification. We have used this approach to isolate human cDNA clones encoding binding proteins of HMN-154 ((E)-4-[2-[2-(p-methoxy-benzene-sulfonamide) phenyl]ethenyl] pyridine), a novel benzenesulfonamide anticancer compound (Katoh and Hidaka 1997). The proteins encoded by two of the isolated clones are identical to NF-YB, B subunit of nuclear transcription factor NF-Y, and thymosin beta-10, respectively. Recombinants of both proteins bind specifically to HMN-154 in vitro. Comparison of amino acid sequences between these proteins shows the sequence similarity in a short amino acid stretch [K(X)AKXXK]. Deletion or mutation of this region causes the significant loss of binding of both proteins to HMN-154. Furthermore, HMN-154 inhibits DNA binding of NF-Y to the human major histocompatibility complex class II human leukocyte antigen DRA Y-box sequence in a dose-dependent manner. Interestingly, other binding proteins identified by this method also possess the same or a similar motif. These results clearly demonstrate that NF-YB and thymosin beta-10 are specific cellular binding proteins of HMN-154 and that this shared region is necessary for the binding to HMN-154. Hence, this new method is thought to be useful for the identification of drug-binding proteins.