ML 349
目录号 : GC17889
A selective and reversible inhibitor of LYPLA2
Cas No.:890819-86-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
Cells are plated in 96-well plates with a density of 4000 to 8000 cells per well and incubated for 24 h at 37°C with 5% CO2. Then cells are treated with increasing drug (including ML349) concentrations and their combinations. Cell viability is measured with the cell viability assay according to the manufacturer's protocol[3]. |
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References: [1]. Won SJ, et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Dec 16;11(12):3374-3382. |
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ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
ML349 is an inhibitor of acyl protein thioesterase 1 and 2 (APT-1 and APT-2) with Kis of >10000 and 120±20 nM, respectively[1]. ML349 is also an inhibitor of both LYPLA1 and LYPLA2 with IC50s of >3000 and 144 nM, respectivley[2]. ML348 and ML349 do not decrease cell viability, but they lead to a slight activation of AKT in NRAS mutant cells[3].
References:
[1]. Won SJ, et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Dec 16;11(12):3374-3382.
[2]. Adibekian A, et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).
[3]. Vujic I, et al. Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitors palmostatin B, ML348 and ML349 have different effects on NRAS mutant melanoma cells. Oncotarget. 2016 Feb 9;7(6):7297-306.
| Cas No. | 890819-86-0 | SDF | |
| 化学名 | (5,5-dioxido-4H-thieno[3,2-c]thiochromen-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone | ||
| Canonical SMILES | COC1=CC=C(N2CCN(C(C3=CC4=C(C(C=CC=C5)=C5S(C4)(=O)=O)S3)=O)CC2)C=C1 | ||
| 分子式 | C23H22N2O4S2 | 分子量 | 454.56 |
| 溶解度 | 5mg/mL in DMSO, or in DMF | 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 | 2.1999 mL | 10.9996 mL | 21.9993 mL |
| 5 mM | 0.44 mL | 2.1999 mL | 4.3999 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.1999 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。