(+)SHIN2
Based on 2 publication(s) in Google Scholar
(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519). (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.30%
- CAS 番号: 3056942-19-6
- 分子式: C23H26N4O3
- 分子量:406.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 (+)SHIN2
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生物活性
Serine hydroxymethyltransferase (SHMT)[1]
(+)SHIN2 (0-10 μM; 24 h) blocks proliferation of HCT116 Ras-driven colon cancer cells, in a stereoselective manner with an IC50 value of 300 nM[1].
(+)SHIN2 (0-100 μM; 48 h) achieves a nearly complete blockade of SHMT activity as evidenced by the decrease in M+1 and M+2 serine, M+2 glycine, and the incorporation of serine-derived glycine and 1C units into ATP, GTP, and dTTP (M+1-M+4 ATP and GTP and M+1 dTTP), and inhibits human T-ALL cell line Molt4 growth with a IC50 value of 89 nM[1].
(+)SHIN2 (2 μM; 24 h) arrests cell cycle at S phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (10-14 weeks old) with mouse primary T-ALL[1]
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Dosage:200 mg/kg
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Administration:Intraperitoneal injection; prepared with 30 mM U-13C-Serine (0.1 μL/min/g; infusion by catheter implanted on the right jugular vein); tested at 8 hr after treatment
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Result:Decreased thymus weight and cellularity, which normalized after treatment discontinuation.
Showed generally well tolerated activity with modest hematological toxicity.
化学情報
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CAS 番号 3056942-19-6
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性状 Solid
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分子量 406.48
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分子式 C23H26N4O3
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Color White to light yellow
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SMILES
N#CC([C@@]1(C2=CC(C#CCCCO)=CC(CO)=C2)C(C)C)=C(N)OC3=C1C(C)=NN3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Res
H4K20me3-Mediated Repression of Inflammatory Genes Is a Characteristic and Targetable Vulnerability of Persister Cancer Cells. [Abstract]2025 Jan 2;85(1):32-51. PMID: 39476057 -
Arch Biochem Biophys
SHIN-2 exerts potent activity against VanA-type vancomycin-resistant Enterococcus faecium in vitro by stabilizing the active site loop of serine hydroxymethyltransferase. [Abstract]2024 Nov:761:110160. PMID: 39313141
溶剤 & 溶解度
DMSO : 100 mg/mL (246.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL | 61.5036 mL |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | 12.3007 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 mL | 6.1504 mL | |
| 15 mM | 0.1640 mL | 0.8200 mL | 1.6401 mL | 4.1002 mL | |
| 20 mM | 0.1230 mL | 0.6150 mL | 1.2301 mL | 3.0752 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9841 mL | 2.4601 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0501 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5376 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2301 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6150 mL |
(+)SHIN2 関連分類
HY-134978A 関連分類
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