Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
K02288 (K-02288; K 02288) is a potent, 2-aminopyridine-based and selective small molecule inhibitor of the BMP (bone morphogenetic protein) signaling pathway with the potential to treat the progressively debilitating musculoskeletal disease fibrodysplasia ossificans progressiva (FOP). It inhibits ALK2 (activin receptor-like kinase-2), ALK1 and ALK6 with IC50s of 1.1, 1.8, 6.4 nM, respectively.
ln Vitro |
K02288 exhibits an apparent IC50 of 100 nM in reducing the strong phosphorylation of Smad1/5/8 induced by BMP4 stimulation. Smad2 phosphorylation is nearly entirely inhibited by K02288 at 0.5 μM [1]. With two hydrogen bonds attached to the kinase hinge, K02288 binds to ALK1 in a manner reminiscent of ATP. In HUVECs, K02288 also causes a hypergermination phenotype and inhibits BMP9-ALK1 signaling [2].
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ln Vivo |
In the chick embryo CAM model, K02288 (1 μM) promotes defective angiogenesis [2].
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Animal Protocol |
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References |
[1]. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721.
[2]. Kerr G, et al. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17. |
Molecular Formula |
C20H20N2O4
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Molecular Weight |
352.38
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CAS # |
1431985-92-0
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Related CAS # |
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SMILES |
OC1=CC=CC(C2=CC(C3=CC(OC)=C(OC)C(OC)=C3)=C(N)N=C2)=C1
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Chemical Name |
3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol
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Synonyms |
K02288; K 02288; K-02288
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.