货号:A189537
同义名:
6-巯基嘌呤一水合物
/ 6-Mercaptopurine monohydrate; Mercaptopurine hydrate
6-Mercaptopurine hydrate 作为嘌呤类似物,竞争性拮抗内源性嘌呤代谢。需经细胞内酶(如次黄嘌呤-鸟嘌呤磷酸核糖转移酶,HGPRT)激活,转化为6-硫代鸟嘌呤核苷酸(6-TGNs),整合到核酸中取代嘌呤碱基,干扰DNA/RNA合成,导致细胞周期阻滞和凋亡。


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|---|---|---|---|---|---|---|---|
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| 产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Fexinidazole | ✔ | 98% | |||||||||||||||||
| Daptomycin | ✔ | 98% | |||||||||||||||||
| Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
| Metronidazole | ✔ | 98% | |||||||||||||||||
| Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
| Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
| Nedaplatin | ✔ | 99%+ | |||||||||||||||||
| Oxolinic acid | ✔ | 98+% | |||||||||||||||||
| Bendamustine | ✔ | 98+% | |||||||||||||||||
| Trifluridine | ✔ | 98% | |||||||||||||||||
| Robinetin | ✔ | 99%+ | |||||||||||||||||
| Carboplatin | ✔ | 99% | |||||||||||||||||
| Cidofovir | ✔ | 99% | |||||||||||||||||
| Cisplatin | ✔ | 99% | |||||||||||||||||
| Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
| Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
| Oxaliplatin | ✔ | 98% | |||||||||||||||||
| YK-4-279 | ✔ | 99%+ | |||||||||||||||||
| ML216 |
+
BLM636-1298, IC50: 0.97 μM BLMfull-length, IC50: 2.98 μM |
99%+ | |||||||||||||||||
| RK-33 | ✔ | 98% | |||||||||||||||||
| Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
| Phen-DC3 Trifluoromethanesulfonate | ✔ | 95% | |||||||||||||||||
| Favipiravir | ✔ | 99% | |||||||||||||||||
| Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
| Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
| Didox | ✔ | 98% | |||||||||||||||||
| (E)-3-AP | ✔ | 99% | |||||||||||||||||
| Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
| BC-LI-0186 |
+++
Leucyl-tRNA synthetase, IC50: 46.11 nM Leucyl-tRNA synthetase, Kd: 42.1 nM |
98% | |||||||||||||||||
| SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | 6-Mercaptopurine Monohydrate is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug. 6-MP induced G2/M arrest, delayed S-phase progression, and finally induced apoptosis of neural progenitor cells mediated by p53 in the fetal rat telencephalon[3]. The thiopurine drugs azathioprine and 6-mercaptopurine (6-MP) are well-established in the treatment of inflammatory bowel disease (IBD) [4]. The mode of action of azathioprine is thought to be multifactorial, including conversion to 6-mercaptopurine (which acts as a purine antimetabolite), possible blockade of thiol groups by alkylation, inhibition of several pathways in nucleic acid biosynthesis (preventing proliferation of cells involved in the determination and amplification of the immune response) and damage to DNA through the incorporation of thiopurine analogues. Azathioprine and 6-mercaptopurine are further known to alter lymphocyte function, reduce the number of lamina propria plasma cells and affect natural killer cell function[5]. 6-Mercaptopurine monohydrate (6-MP) was administered intraperitoneally (i.p.) or orally (p.o.) to 2 strains of mice, MS/Ae and CD-1. From the results of an acute toxicity test and a pilot micronucleus test, the doses selected for the final micronucleus test were 12.5-100 mg/kg for the i.p. route and 25-200 mg/kg for the p.o. route[6]. |
| Concentration | Treated Time | Description | References | |
| MES28 cells | 10 μM | 2 h | 6-MP competitively inhibits HPRT1 activity, blocks TMZ-induced AMPK activation and RRM1 T52 phosphorylation, thereby enhancing TMZ sensitivity in glioblastoma cells | Nat Commun. 2023 Sep 22;14(1):5913. |
| U87 cells | 10 μM | 2 h | 6-MP competitively inhibits HPRT1 activity, blocks TMZ-induced AMPK activation and RRM1 T52 phosphorylation, thereby enhancing TMZ sensitivity in glioblastoma cells | Nat Commun. 2023 Sep 22;14(1):5913. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Abcc4−/− mice | 100 mg/kg | Daily administration for 10 days | To study the role of ABCC4 in protecting megakaryocytes from 6-Mercaptopurine toxicity, results showed that Abcc4?/? mice had a significant reduction in megakaryocytes and impaired platelet production after 6-MP treatment. | Drug Resist Updat. 2024 Jan;72:101017 | |
| Nude mice | Intracranial glioblastoma model | Intraperitoneal injection | 20 mg/kg | 5 consecutive days | Combined treatment with 6-MP and TMZ significantly inhibits tumor growth, prolongs mouse survival, and enhances TMZ-induced DNA damage and apoptosis | Nat Commun. 2023 Sep 22;14(1):5913. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00819351 | Acute Lymphoblastic Leukemia | Phase 3 | Completed | - | Denmark ... 展开 >> Department of Pediatrics, Rigshospitalet Copenhagen, Denmark, 2100 Finland Helsinki University Hospital Helsinki, Finland Iceland University Hospital Reykjavik, Iceland Reykjavik, Iceland Norway Trondheim University Hospital Trondheim, Norway Sweden Department of Pediatrics, Drottning Sylvias Pediatric Hospital Gothenburg, Sweden NOPHO nordic organisation for pediatric onology Stockholm, Sweden 收起 << |
| NCT00609973 | - | Completed | - | - | |
| NCT01458951 | Ulcerative Colitis | Phase 3 | Completed | - | - |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
5.88mL 1.18mL 0.59mL |
29.38mL 5.88mL 2.94mL |
58.76mL 11.75mL 5.88mL |
|
| CAS号 | 6112-76-1 |
| 分子式 | C5H6N4OS |
| 分子量 | 170.19 |
| SMILES Code | SC1=C2NC=NC2=NC=N1.[H]O[H] |
| MDL No. | MFCD03854445 |
| 别名 | 6-巯基嘌呤一水合物 ;6-Mercaptopurine monohydrate; Mercaptopurine hydrate; 6-MP; 6-Mercaptopurine (hydrate); 6-MP hydrate |
| 运输 | 蓝冰 |
| InChI Key | WFFQYWAAEWLHJC-UHFFFAOYSA-N |
| Pubchem ID | 2724350 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, room temperature |
| 溶解方案 |
DMSO: 50 mg/mL(293.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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