Arcyriaflavin A
目录号 : GC13649
A CDK4 and CAMKII inhibitor
Cas No.:118458-54-1
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
IC50: 0.2 μM for HCMV [1], 0.14 μM for D1–CDK4 [2]
The natural product Arcyriaflavin A, unsubstituted indolocarbazole, was a potent selective inhibitor of human cytomegalovirus (HCMV) replication. HCMV infection is typically unnoticed in healthy people, but can be life-threatening for the immunocompromised.
In vitro: Arcyriaflavin A is a potent, selective inhibitor of HCMV replication in cell culture, and the anti-HCMV activity appeared no relation to the inhibition of protein kinase C. The imide NH was identified to be essential for anti-HCMV activity [1]. Arcyriaflavin A also has been showed the inhibitory activity against D1/CDK4 with a IC50 of 59 nM. Based on X-ray co-crystal structure of staurosporine and the human CDK2, the acidic proton of the maleimide moiety and the carbonyl group play critical roles by acting as a hydrogen bond donor and acceptor in the ATP binding pocket of CDK2 [2].
In vivo: So far, no in vivo study has been conducted.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Slater MJ, Cockerill S, Baxter R, Bonser RW, Gohil K, Gowrie C, Robinson JE, Littler E, Parry N, Randall R, Snowden W. Indolocarbazoles: potent, selective inhibitors of human cytomegalovirus replication. Bioorg Med Chem. 1999 Jun;7(6):1067-74.
[2] Zhu G, Conner S, Zhou X, Shih C, Brooks HB, Considine E, Dempsey JA, Ogg C, Patel B, Schultz RM, Spencer CD, Teicher B, Watkins SA. Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1231-5.
| Cas No. | 118458-54-1 | SDF | |
| 化学名 | 12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione | ||
| Canonical SMILES | O=C(C1=C2C(NC3=CC=CC=C23)=C4NC5=CC=CC=C5C4=C16)NC6=O | ||
| 分子式 | C20H11N3O2 | 分子量 | 325.32 |
| 溶解度 | DMF: 5 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 1 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 | 3.0739 mL | 15.3695 mL | 30.739 mL |
| 5 mM | 0.6148 mL | 3.0739 mL | 6.1478 mL |
| 10 mM | 0.3074 mL | 1.5369 mL | 3.0739 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。