MS37452 |
Catalog No.GC12630
One-Click Copy Product Info
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MS37452는 27.7μM의 Kd로 H3K27me3에 결합하는 CBX7 크로모도메인의 강력한 억제제입니다. MS37452는 전립선암 세포에서 INK4A/ARF 유전자좌에 대한 CBX7 결합을 대체함으로써 폴리콤 억제 복합 표적 유전자 p16/CDKN2A의 전사를 억제할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 423748-02-1
Sample solution is provided at 25 µL, 10mM.
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Ki = 43 μM
MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3.
Chromobox homolog 7 (CBX7) functions via its N-terminal chromodomain, which recognizes histone 3 trimethyl lysine 27 (H3K27me3), to repress gene transcription. Chromobox homolog 7 plays a critical role in gene transcription in cellular processes associated with stem cell differentiation and self-renewal, as well as tumor progression.
In vitro: In a previous study, the crystal structures revealed the binding modes of MS37452 and its close analogs that competed against H3K27me3 binding via interactions with key residues in the methyl-lysine binding pocket of CBX7ChD. It was further found that MS37452 as the lead compound was able to derepress the transcription of Polycomb repressive complex target gene p16/CDKN2A through displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells. These findings showed that MS37452 and its close analogs had the potential to be developed into high-potency chemical modulators targeting CBX7 functions in gene transcription in various disease pathways [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Ren, C. ,Morohashi, K.,Plotnikov, A.N., et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chemistry & Biology 22, 161-168 (2015).
| Cas No. | 423748-02-1 | SDF | |
| Chemical Name | 1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-ethanone | ||
| Canonical SMILES | COC1=CC=CC(C(N2CCN(C(COC3=CC(C)=CC=C3)=O)CC2)=O)=C1OC | ||
| Formula | C22H26N2O5 | M.Wt | 398.5 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.5094 mL | 12.5471 mL | 25.0941 mL |
| 5 mM | 501.9 μL | 2.5094 mL | 5.0188 mL |
| 10 mM | 250.9 μL | 1.2547 mL | 2.5094 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)