K02288 |
| カタログ番号GC15567 |
K02288 は強力な骨形成タンパク質 (BMP) I 型受容体阻害剤で、ALK1、ALK2、ALK6 の IC50 はそれぞれ 1.8、1.1、6.4 nM です。
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Cas No.: 1431985-92-0
Sample solution is provided at 25 µL, 10mM.
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K02288 is a highly selective inhibitor of ALK2 with IC50 value of 1.1nM [1].
K02288 is a 2-aminopyridine inhibitor of ALK2. It shows high selectivity for the homologous kinases ALK1-6 and ActRIIA. K02288 shows potency against the type I BMP receptors ALK1, ALK2 (IC50s range from 1–2nM), ALK3 and ALK6 (IC50s of 5–34nM), ALK4 (IC50 of 302nM) and ALK5 (IC50 of 321nM). K02288 has a favorable kinome-wide selectivity. In a panel of 200 human kinases, it shows more than 50% inhibition against only ABL and ARG at 0.1μM and only a further 6 kinases at 1μM [1].
K02288 also affects ALK2 related BMP signaling. In C2C12 cells, it reduces the phosphorylation of Smad dose-dependently when using BMP4 or BMP6 as ligands. Furthermore, K02288 induces a dorsalized phenotype in Tg(BRE:mRFP) transgenic zebrafish embryos [1].
References:
[1] Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721.
| Cas No. | 1431985-92-0 | SDF | |
| Chemical Name | 3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol | ||
| Canonical SMILES | COC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N | ||
| Formula | C20H20N2O4 | M.Wt | 352.38 |
| 溶解度 | ≥ 17.6mg/mL in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8378 mL | 14.1892 mL | 28.3785 mL |
| 5 mM | 0.5676 mL | 2.8378 mL | 5.6757 mL |
| 10 mM | 0.2838 mL | 1.4189 mL | 2.8378 mL |
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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.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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