| Size | Price | Stock | Qty |
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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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Purity: ≥98%
Pluripotin (also known as SC1; SC-1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP as well as a sustainer of mES self-renewal. With an EC50 of 2.5±1.8 μM, pluripotin inhibits the in vitro kinase activity of RSK2. It keeps embryonic stem cells' (ESC) ability to renew itself. SC1 has an impact on mES cells only when both protein activities are simultaneously inhibited, which is both necessary and sufficient. Ras is activated by SC1 by blocking RasGAP activity. The C57BL/6-derived ES cells' derivation effectiveness and pluripotency were enhanced by SC1. When cultured with SC1, three different pluripotent stem cell types (fES, ntES, and iPS cells) of the C57BL/6 background were highly effective at producing full-term pups.
| Targets |
ERK1 (Kd = 98 nM); RasGAP (Kd = 212 nM); RSK1 (Kd = 0.5 μM); RSK2 (Kd = 2.5 μM); RSK3 (Kd = 3.3 μM); RSK4 (Kd = 10 μM)
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| ln Vitro |
SC1 is a dual-purpose small molecule inhibitor of ERK1 and RasGAP, and it only affects mES cells when both protein activities are simultaneously inhibited. Ras is activated by SC1 by blocking RasGAP function[1]. The C57BL/6-derived ES cells' derivation efficiency and pluripotency were enhanced by SC1. When cultured with SC1, three different types of pluripotent stem cells (fES, ntES, and iPS cells) with a C57BL/6 background were highly efficient at producing full-term pups[1].
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| ln Vivo |
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| Enzyme Assay |
Pluripotin (SC-1) inhibits in vitro kinase activity of RSK2 with EC50 of 2.5±1.8 μM. The RSK2 in vitro kinase inhibition assay used was a modification of the guidelines set forth by Nguyen et al. At Reaction Biology Corporation (Malvern, PA), additional protocols that verified the outcomes shown in Figure 4 and assessed kinase inhibitory activity in a randomly chosen protein kinase were carried out. It was a miniature 33P-based screening assay.
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| Cell Assay |
mES cells are plated in six-well gelatin-coated plates at a density of 1.6×104 cells/cm2 and maintained with 3 μM SC1 in ESC-SR media, 1 μM SC1 in ESC-N2B27 media, or 300 nM SC1 in ESC-N2 media without LIF or feeder cells. As a positive control, mES cells maintained in ESC-N2B27 media with 103 units/ml LIF and 10 ng/ml BMP4 are used. As negative controls, mES cells are exposed to DMSO for two passages in ESC-SR, ESC-N2B27, or ESC-N2 media. Every three days, cells are divided and seeded at the same density (1.6×104 cells/cm2). FACS, immunocytochemistry, histocytochemistry, and RT-PCR are used to examine mES cells at passage 11.
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| Animal Protocol |
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| References |
| Molecular Formula |
C27H25F3N8O2
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| Molecular Weight |
550.53
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| Exact Mass |
550.21
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| Elemental Analysis |
C, 58.90; H, 4.58; F, 10.35; N, 20.35; O, 5.81
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| CAS # |
839707-37-8
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)N3CC4=CN=C(N=C4N(C3=O)C)NC5=CC(=NN5C)C
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| InChi Key |
NBZFRTJWEIHFPF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H25F3N8O2/c1-15-8-9-20(32-24(39)17-6-5-7-19(11-17)27(28,29)30)12-21(15)38-14-18-13-31-25(34-23(18)36(3)26(38)40)33-22-10-16(2)35-37(22)4/h5-13H,14H2,1-4H3,(H,32,39)(H,31,33,34)
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| Chemical Name |
N-[3-[7-[(2,5-dimethylpyrazol-3-yl)amino]-1-methyl-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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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 (4.54 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 (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8164 mL | 9.0822 mL | 18.1643 mL | |
| 5 mM | 0.3633 mL | 1.8164 mL | 3.6329 mL | |
| 10 mM | 0.1816 mL | 0.9082 mL | 1.8164 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.
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