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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%
RepSox (also called E-616452, SJN-2511; E 616452; SJN 2511, and ALK5 Inhibitor II) is a potent, cell permeable, and selective inhibitor of the TGFβR-1/ALK5 (transforming growth factor-beta type I receptor, ALK5) with important biological activity. It inhibits TGFβR-1/ALK5 with an IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively. RepSox slows the decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. RepSox inhibited ALK5 autophosphorylation with IC50 = 6 and 4 nM, respectively, showed potent activities in both binding and cellular assays and exhibited selectivity over p38 mitogen-activated protein kinase.
ln Vitro |
MEFs are induced to differentiate into chemically induced pluripotent stem cells (CiPSCs) by RepSox (GMP) (10 μM)[1]. hCiPS cells are induced from HEFs by RepSox (GMP) (10 μM, in stage I-Stage III induction medium)[2]. Increased EdU incorporation confirms that RepSox (GMP) plus Forskolin boost the number of proliferative cells in MEFs expressing MyoD[3].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Zhao T, et al. Single-Cell RNA-Seq Reveals Dynamic Early Embryonic-like Programs during Chemical Reprogramming. Cell Stem Cell. 2018 Jul 5;23(1):31-45.e7.
[2]. Guan J, et al. Chemical reprogramming of human somatic cells to pluripotent stem cells. Nature. 2022 May;605(7909):325-331. [3]. Bar-Nur O, et al. Direct Reprogramming of Mouse Fibroblasts into Functional Skeletal Muscle Progenitors. Stem Cell Reports. 2018 May 8;10(5):1505-1521. |
Molecular Formula |
C17H13N5
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Molecular Weight |
287.32
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CAS # |
446859-33-2
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Related CAS # |
RepSox;446859-33-2
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SMILES |
CC1=CC=CC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=N1
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Chemical Name |
2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine
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Synonyms |
E-616452, SJN 2511; E 616452; E616452; RepSox; SJN-2511; SJN-2511; ALK5 Inhibitor II
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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: ≥ 7.5 mg/mL (26.10 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 75.0 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: ≥ 7.5 mg/mL (26.10 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 75.0 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: ≥ 1.67 mg/mL (5.81 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 1.67 mg/mL (5.81 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. Solubility in Formulation 5: ≥ 0.33 mg/mL (1.15 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4804 mL | 17.4022 mL | 34.8044 mL | |
5 mM | 0.6961 mL | 3.4804 mL | 6.9609 mL | |
10 mM | 0.3480 mL | 1.7402 mL | 3.4804 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.