[CAS NO. 1181770-72-8] EMD638683

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PRODUCTS SPECIFICATIONS [1181770-72-8]

Catalog

HY-15193

Brand

MCE

CAS

1181770-72-8

DESCRIPTION [1181770-72-8]

Overview

MDL	MFCD25541743
Molecular Weight	364.34
Molecular Formula	C18H18F2N2O4
SMILES	CC1=C(CC)C(C(NNC(C(O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O

For research use only. We do not sell to patients.

12 Publications Citing Use of MCE

Summary

EMD638683 is a highly selective SGK1 inhibitor, with an IC ₅₀ value of 3 μM.

IC50 & Target

SGK1

In Vitro

EMD638683 is a SGK1 inhibitor. EMD638683 inhibits the NDRG1 (N-Myc downstream-regulated gene 1) phosphorylation, an effect requiring 3.35±0.32 μM EMD638683 in the cell culture medium for half maximal effect (IC ₅₀ ). EMD638683 has also an inhibitory effect on cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), and the SGK isoforms SGK2 and SGK3 ^[1] . In both, control and EMD638683 (50 µM)-treated CaCo-2 cells, radiation significantly increases the percentage of CaCo-2 cells undergoing late apoptosis. EMD638683 treatment alone tends to enhance the percentage of apoptotic CaCo-2 cells. Following radiation the percentage of apoptotic EMD638683-treated CaCo-2 cells is significantly higher than the percentage of apoptotic control cells. Thus, EMD638683 treatment significantly augments the apoptosis following radiation ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The colon is significantly longer and the colon weight significantly lower in EMD638683-treated mice than in placebo-treated mice, a finding pointing to an influence of EMD638683 on tumor growth following chemical carcinogenesis. In addition, the stomach weight is significantly lower in the EMD treated group. Most importantly, the number of developing tumors following carcinogenic treatment is significantly blunted by EMD638683 treatment ^[2] . EMD638683 (20 mg/kg, intragastrically) prevents progression of monocrotaline (MCT)-induced pulmonary vascular remodeling in rats. Hemodynamic characteristics show that EMD638683 treatment attenuates right ventricular systolic pressure (RVSP) (15.8±2.5 vs. 28.2±3.1 mmHg; P<0.05; n=6) and right ventricular hypertrophy index (RVHI) (0.27±0.02 vs. 0.41±0.06;P<0.05; n=6) compare to vehicle-dosed controls ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL ( 137.23 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7447 mL	13.7234 mL	27.4469 mL
5 mM	0.5489 mL	2.7447 mL	5.4894 mL
10 mM	0.2745 mL	1.3723 mL	2.7447 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

* All of the co-solvents are available by MCE.