KDM4-IN-2
Based on 1 Customer Validation
KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.
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 : 98.29%
- CAS 番号: 2369607-62-3
- 分子式: C25H26N6O
- 分子量:426.51
-
保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-12304
IOX12OG Oxygenases Inhibitor -
HY-15648B
GSK-J4JMJD3/UTX Inhibitor -
HY-100421
CPI-455KDM5 Inhibitor -
HY-15648
GSK-J1JMJD3/KDM6B Inhibitor -
HY-12635
SP2509LSD1 Antagonist -
HY-13953
JIB-04Histone Demethylase Inhibitor -
HY-101799
NCGC00244536KDM4B Inhibitor -
HY-116761
GSK467KDM5B Inhibitor -
HY-107573
KDM2/7-IN-1KDM2/7 Inhibitor -
HY-18632
GSK2879552LSD1 Inhibitor -
HY-108706
KDM2A/7A-IN-1Histone Demethylase Inhibitor -
HY-100422
KDM5-IN-1KDM5 Inhibitor
生物活性
製品説明
IC50 & Target
|
KDM4 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
13.4 μM
Compound: 19a
|
Inhibition of full length human wild type KDM5B transfected in HeLa cells assessed as decrease in demethylation of H3K4Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
Inhibition of full length human wild type KDM5B transfected in HeLa cells assessed as decrease in demethylation of H3K4Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
|
[PMID: 31158747] |
| HeLa | EC50 |
4.7 μM
Compound: 19a
|
Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
|
[PMID: 31158747] |
| Sf9 | IC50 |
0.043 μM
Compound: 19a
|
Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG
Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG
|
[PMID: 31158747] |
化学情報
-
CAS 番号 2369607-62-3
-
性状 Solid
-
分子量 426.51
-
分子式 C25H26N6O
-
Color Light yellow to yellow
-
SMILES
O=C1C2=CC=NC(N3C=C(CCN4CCC5(CCC6=C5C=CC=C6)CC4)C=N3)=C2N=CN1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外:
DMSO : 4 mg/mL (9.38 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 and light). 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 and light). 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
-
データシート (275 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Le Bihan YV, et al. C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. Eur J Med Chem. 2019 Sep 1;177:316-337. [Content Brief]
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 and light). 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 | 2.3446 mL | 11.7231 mL | 23.4461 mL | 58.6153 mL |
| 5 mM | 0.4689 mL | 2.3446 mL | 4.6892 mL | 11.7231 mL |
KDM4-IN-2 関連分類
HY-128343 関連分類
Powered by Bioz