应用
该试剂盒既可用于检测DHFR活性，也可用于筛选和DHFR抑制剂。检测原理为NADPH的DHFR能够可逆催化二氢叶酸还原为四氢叶酸，再通过监测340nm处吸光度降低情况就可以跟踪反应进程。
二氢叶酸+ NADPH+H+↔四氢叶酸+NADP+
二氢叶酸+ NADPH+H+↔四氢叶酸+NADP+
生化/生理作用
DHFR（二氢叶酸还原酶）是一种在核苷酸碱基反应中催化生物合成DNA所必需的酶。阻断该酶就会抑制DNA合成，最终导致细胞死亡。因此DHFR也是抗肿瘤药物的出色靶点。
特点和优势
- 操作方法快速、简便。
- 包含比色法测定DHFR活性所需的全部试剂，适用于细胞裂解物、组织匀浆或酶纯化柱组分。
- 包含纯化酶，可用作阳性对照或用于筛选DHFR抑制剂。
- 包含甲氨蝶呤（MTX），后者是一种原核和真核的DHFR特异性抑制剂，具有抗肿瘤活性。
- 已经在A431、NIH-3T3、CHO细胞系，大鼠肝、肾、脑和骨骼肌组织提取物，以及重组DHFR中进行测试。
仅试剂盒组分
产品编号
说明
- Assay Buffer 10x for DHFR 30 mL
- Dihydrofolate Reductase (DHFR) human .1 U
- Dihydrofolic acid (DHFR substrate) 3 x 10
- Amethopterin (+)(methotrexate, MTX)
(DHFR inhibitor) 2 x 10 - NADPH (β-Nicotinamide adenine dinucleotide phosphate reduced tetrasodium salt) 25 mg
警示用语：
Danger
危险分类
Acute Tox. 3 Oral - Eye Irrit. 2 - Repr. 1B - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
常规特殊物品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Bharath Srinivasan et al.
The FEBS journal, 282(10), 1922-1938 (2015-02-24)
Dihydrofolate reductase (DHFR) is a pivotal enzyme involved in the de novo pathway of purine synthesis, and hence, represents an attractive target to disrupt systems that require rapid DNA turnover. The enzyme acquires resistance to available drugs by various molecular
Amrinder Singh et al.
Scientific reports, 8(1), 3190-3190 (2018-02-18)
We report the first peptide based hDHFR inhibitors designed on the basis of structural analysis of dihydrofolate reductase (DHFR). A set of peptides were rationally designed and synthesized using solid phase peptide synthesis and characterized using nuclear magnetic resonance and
Em Canh Pham et al.
ACS omega, 7(37), 33614-33628 (2022-09-27)
Naphthamide is a common structural framework with diverse pharmacological activities. Ten novel 2-naphthamide derivatives have been designed, synthesized, and evaluated for their in vitro antibacterial, antifungal, and anticancer activities. The title compounds were synthesized from dimethoxybenzaldehyde derivatives through a four-step
Piermichele Kobauri et al.
Journal of medicinal chemistry, 65(6), 4798-4817 (2022-03-09)
Photopharmacology uses light to regulate the biological activity of drugs. This precise control is obtained through the incorporation of molecular photoswitches into bioactive molecules. A major challenge for photopharmacology is the rational design of photoswitchable drugs that show light-induced activation.
Bermans J Iskandar et al.
The Journal of clinical investigation, 120(5), 1603-1616 (2010-04-29)
The folate pathway plays a crucial role in the regeneration and repair of the adult CNS after injury. Here, we have shown in rodents that such repair occurs at least in part through DNA methylation. In animals with combined spinal
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