MS67
Based on 1 Customer Validation
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
(Pink: WDR5 ligand (HY-184594); Blue: VHL ligand (HY-112078); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.12%
- CAS 番号: 2407452-77-9
- 分子式: C52H59F4N9O7S
- 分子量:1030.14
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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生物活性
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VHL |
WDR5 63 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | GI50 |
>2500 nM
Compound: MS67
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Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
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[PMID: 38085679] |
| MV4-11 | GI50 |
15 nM
Compound: MS67
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Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
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[PMID: 38085679] |
MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells[1].
MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin[1].
The GI50 values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67[1].
. MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a Kd of 140 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4;11 cells
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Concentration:0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM
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Incubation Time:18 hours
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Result:Induced WDR5 degradation at a concentration as low as 1 nM with DC50 of 3.7 nM.
After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4;11 MLL-r AML xenograft mouse[1]
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Dosage:75 mg/kg
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Administration:i.p.; twice daily; 5 days a week; for 20 days
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Result:Inhibited tumor growth in vivo.
化学情報
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CAS 番号 2407452-77-9
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性状 Solid
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分子量 1030.14
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分子式 C52H59F4N9O7S
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Color White to off-white
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SMILES
O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3C[C@H](N([C@H](C3)C)C)C)C=CC(C4=CC(C(NCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O)=O)=CC=C4F)=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (97.07 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
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- 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 (sealed storage, away from moisture). 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 | 0.9707 mL | 4.8537 mL | 9.7074 mL | 24.2685 mL |
| 5 mM | 0.1941 mL | 0.9707 mL | 1.9415 mL | 4.8537 mL | |
| 10 mM | 0.0971 mL | 0.4854 mL | 0.9707 mL | 2.4269 mL | |
| 15 mM | 0.0647 mL | 0.3236 mL | 0.6472 mL | 1.6179 mL | |
| 20 mM | 0.0485 mL | 0.2427 mL | 0.4854 mL | 1.2134 mL | |
| 25 mM | 0.0388 mL | 0.1941 mL | 0.3883 mL | 0.9707 mL | |
| 30 mM | 0.0324 mL | 0.1618 mL | 0.3236 mL | 0.8090 mL | |
| 40 mM | 0.0243 mL | 0.1213 mL | 0.2427 mL | 0.6067 mL | |
| 50 mM | 0.0194 mL | 0.0971 mL | 0.1941 mL | 0.4854 mL | |
| 60 mM | 0.0162 mL | 0.0809 mL | 0.1618 mL | 0.4045 mL | |
| 80 mM | 0.0121 mL | 0.0607 mL | 0.1213 mL | 0.3034 mL |
MS67 関連分類
HY-141796 関連分類
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