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Purity: ≥98%
EMD638683 is a potent inhibitor of SGK1 with an IC50 of 3 μM. EMD638683 treatment significantly augmented the radiation-induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis. EMD638683 promotes radiation-induced suicidal death of colon tumor cells in vitro and decreases the number of colonic tumors following chemical carcinogenesis in vivo.
| ln Vitro |
EMD638683 is a conjugate of SGK1. Half-maximum effect (IC50) of EMD638683's inhibition of NDRG1 (N-Myc downstream regulatory gene 1) needs the addition of 3.35 μM EMD638683 to the cell culture medium. Moreover, three cAMP topologies in control and EMD638683 (50 μM) are inhibited by EMD63868: SGK isoforms SGK2 and SGK3, mitogen- and casein-activated protein kinase 1 (MSK1), and protein kinase C-related protein kinase 2 (PKR2) [1]. irradiation markedly raised the proportion of CaCo-2 cells treated with late cells. ) treated CaCo-2 cells. The percentage of CaCo-2 cells tended to rise with treatment with EMD638683 alone. A small number received EMD638683 treatment following radiation. In light of this, EMD638683 therapy greatly increased UV radiation following irradiation [2].
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| ln Vivo |
In comparison to the night-treated group, the EMD638683-treated group's night weight was much lower and its night length was significantly longer. This result suggests that, following chemical action, EMD638683 has an impact on tumor growth. Additionally, the group receiving EMD treatment saw a considerable decrease in stomach weight. was given EMD638683 treatment, which considerably lowered the quantity of tumors that grew as a result of food processing [2]. In lung cancer patients, monocrotaline (MCT)-guided vascular transplantation is stopped from progressing by EMD638683 (20 mg/kg, gavage). According to the hemodynamic profile, the EMD638683 therapy was found to lower the right ventricular hypertrophy index (RVHI) (0.27 vs. 0.41; P<0.05; n = 6) and right ventricular systolic pressure (15.8 vs. 28.2 mmHg; P<0.05; n = 6) as compared to the control dose [3].
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| References |
[1]. Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-46.
[2]. Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-48. [3]. Xi X, et al. Serum-glucocorticoid regulated kinase 1 regulates macrophage recruitment and activation contributing to monocrotaline-induced pulmonary arterial hypertension. Cardiovasc Toxicol. 2014 Dec;14(4):368-78. [4]. Zhou H, et al. Inhibition of serum- and glucocorticoid-inducible kinase 1 enhances TLR-mediated inflammation and promotes endotoxin-driven organ failure. FASEB J. 2015 Sep;29(9):3737-49 |
| Molecular Formula |
C18H18F2N2O4
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|---|---|
| Molecular Weight |
364.3488
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| Exact Mass |
364.1235
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| CAS # |
1181770-72-8
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| Related CAS # |
EMD638683 R-Form;1184940-47-3;EMD638683 S-Form;1184940-46-2
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| SMILES |
O=C(NNC(C(C1=CC(F)=CC(F)=C1)O)=O)C2=CC=C(O)C(C)=C2CC
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| InChi Key |
SSNAPUUWBPZGOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18F2N2O4/c1-3-13-9(2)15(23)5-4-14(13)17(25)21-22-18(26)16(24)10-6-11(19)8-12(20)7-10/h4-8,16,23-24H,3H2,1-2H3,(H,21,25)(H,22,26)
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| Chemical Name |
N'-[2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide
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| Synonyms |
EMD638683 EMD 638683 EMD-638683.
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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) |
DMSO : ≥ 50 mg/mL (~137.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 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 (6.86 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 (6.86 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 | 2.7446 mL | 13.7231 mL | 27.4461 mL | |
| 5 mM | 0.5489 mL | 2.7446 mL | 5.4892 mL | |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7446 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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