EZM 2302 (Synonyms: GSK3359088) |
رقم الكتالوجGC19149
One-Click Copy Product Info
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EZM 2302 هو مثبط لـ arginine methyltransferase 1 (CARM1) المرتبط بالمُنشّط مع IC50 من 6 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628830-21-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 | |
| المرادفات | 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 | ||
| Formula | C29H37ClN6O5 | M.Wt | 585.09 |
| الذوبان | DMSO : ≥ 125 mg/mL (213.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)