EZM 2302是一种对CARM1有效的且具有选择性的抑制剂，其IC50值为6nM。
Cas No.:1628830-21-6
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
EZM 2302 is a kind of potent and selective inhibitor of CARM1 with an IC50 value of 6nM [1]. EZM 2302 stabilizes an inactive CARM1-S-adenosylhomocysteine (SAH) complex, thereby preventing substrate access and inhibiting methyltransferase activity [1].
EZM 2302 (0~5μM; 96h) led to a concentration-dependent decrease in methylation of PABP1 in the multiple myeloma cell line RPMI-8226; EZM 2302 (0~10μM; 6d) inhibited the proliferation of multiple hematopoietic cell lines [1].
EZM 2302 (37.5, 75, 150 and 300mg/kg; 21d; bid; p.o.) showed significant decreases in tumor growth in CB-17 SCID mice which bore subcutaneous RPMI-8226 xenografts [1]. EZM 2302 (50mg/kg; 11d; i.g.) significantly reduced asymmetrically dimethylated PABP1Arg455/460 content and PABP1 methylation status in C57BL6J/129 mice; EZM 2302 (50mg/kg; 11d; i.g.) decreased the exercise capacity and muscular endurance of male C57BL6J/129 mice [2].
References:
[1] Drew A E, Moradei O, Jacques S L, et al. Identification of a CARM1 inhibitor with potent in vitro and in vivo activity in preclinical models of multiple myeloma [J]. Scientific reports, 2017, 7(1): 17993.
[2] Webb E K, Ng S Y, Mikhail A I, et al. Impact of short-term, pharmacological CARM1 inhibition on skeletal muscle mass, function, and atrophy in mice [J]. American journal of physiology Endocrinology and metabolism, 2023, 325(3): 252-266.
EZM 2302是一种对CARM1有效的且具有选择性的抑制剂，其IC50值为6nM[1]。EZM 2302能通过稳定不活跃的CARM1-S-腺苷基高半胱氨酸（SAH）复合体，从而阻止底物进入并抑制甲基转移酶的活性[1]。
EZM 2302（0~5μM；96h）使多发性骨髓瘤细胞系RPMI-8226中的PABP1甲基化水平呈浓度依赖性下降；EZM 2302（0~10μM；6d）抑制多种造血细胞系的增殖[1]。
EZM 2302（37.5、75、150和300mg/kg；21d；bid；p.o.）显著抑制了皮下移植了RPMI-8226的CB-17 SCID小鼠体内的肿瘤生长[1]。EZM 2302（50mg/kg；11d；i.g.）显著降低C57BL6J/129小鼠的不对称二甲基化PABP1Arg455/460的含量和PABP1甲基化状态；EZM 2302（50mg/kg；11d；i.g.）降低雄性C57BL6J/129小鼠的运动能力和肌肉耐力[2]。
| Cell experiment [1]: | |
Cell lines | Multiple myeloma cell line RPMI-8226 |
Preparation Method | Cells were treated with several concentrations of EZM 2302 for 96h. The cellular methylation was tested by immunoblot, methylation changes were measured by the well-characterized CARM1 substrates PABP1 and SmB and the changes in overall levels of asymmetric dimethyl arginine (aDMA) were assessed with an antibody that detects a generic aDMA motif. |
Reaction Conditions | 0~5μM; 96h |
Applications | EZM 2302 led to a concentration-dependent decrease in methylation of PABP1 and SmB, as well as in multiple aDMA bands. |
| Animal experiment [1]: | |
Animal models | CB-17 SCID mice |
Preparation Method | Mice bearing subcutaneous RPMI-8226 xenografts were received EZM 2302 with twice daily oral dosing on four dose groups. After 21d of continuous dosing, mice were euthanized to collect blood and tissues for methyl mark analysis. |
Dosage form | 37.5, 75, 150 and 300mg/kg; 21d; bid; p.o. |
Applications | EZM 2302 showed significant decreases in tumor growth, decreased the level of methylation at CARM1 substrates with a dose-dependent way in RPMI-8226 xenograft tumors. |
References: | |
| Cas No. | 1628830-21-6 | SDF | |
| 别名 | GSK3359088 | ||
| Canonical SMILES | CNC[C@@H](O)COC1=CC=C(Cl)C(C2=NC(N3CC4(CCN(C(OC)=O)CC4)C3)=C(C)C(C5=C(C)ON=C5C)=N2)=C1 | ||
| 分子式 | C29H37ClN6O5 | 分子量 | 585.09 |
| 溶解度 | DMSO : ≥ 125 mg/mL (213.64 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7091 mL | 8.5457 mL | 17.0914 mL |
| 5 mM | 341.8 μL | 1.7091 mL | 3.4183 mL |
| 10 mM | 170.9 μL | 854.6 μL | 1.7091 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet