2. Anti-infection
  3. Bacterial
  4. GSK2556286

GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes.

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GSK2556286 Chemical Structure

GSK2556286 Chemical Structure

CAS No. : 1210456-20-4

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Based on 1 publication(s) in Google Scholar

GSK2556286 Related Antibodies

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  • Purity & Documentation

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Description

GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes[1][2][3].

IC50 & Target

IC50: 0.07 μM (human macrophage)[1]
In Vitro

GSK2556286 requires the presence of cholesterol to demonstrate activity in axenic culture with IC50 of 2.12 and 0.71 μM in H37Rv and Erdman respectively, whilst the IC50 with glucose medium is >125 and >50 μM in H37Rv and Erdman respectively[2].
GSK2556286 (5 μM, 24 h) increases the intracellular cAMP levels around 50-fold higher in M. tuberculosis lysates than untreated cells only when Rv1625c is expressed[1].
GSK2556286 (10 μM) reduces the amount of 14CO2 released from 14C-cholesterol by 90% and the propionyl-CoA levels in M. tuberculosis when bacteria cultured in cholesterol media supplemented with acetate[1].
GSK2556286 (1 nM-10 μM) exhibits decreased MIC in cholesterol media around 10-fold and decreased concertration required to inhibit GFP signal in wild-type M. tuberculosis overexpressing rv1625c[1].

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

GSK2556286 Related Antibodies
Parmacokinetics
Species Dose SampleTime Route Indicator value
Dog 3 mg/kg p.o. Vss 2.50 L/kg
Dog 5 mg/kg 30 i.v. Vss 2.50 L/kg
Mice 1 mg/kg i.v. CL 9.02 mL/min/kg
Mice 10 mg/kg p.o. CL 9.02 mL/min/kg
Rat 5 mg/kg p.o. CL 34.7 mL/min/kg
Rat 5 mg/kg 30 i.v. CL 34.7 mL/min/kg
Dog 3 mg/kg p.o. T1/2 1.92 hr
Dog 5 mg/kg 30 i.v. T1/2 1.92 hr
Mice 1 mg/kg i.v. Vss 1.76 L/kg
Mice 10 mg/kg p.o. Vss 1.76 L/kg
Rat 5 mg/kg p.o. Vss 2.1 L/kg
Rat 5 mg/kg 30 i.v. Vss 2.1 L/kg
Dog 3 mg/kg p.o. F 51.3 %
Dog 5 mg/kg 30 i.v. F 51.3 %
Mice 1 mg/kg i.v. T1/2 2.47 hr
Mice 10 mg/kg p.o. T1/2 2.47 hr
Rat 5 mg/kg p.o. T1/2 2.31 hr
Rat 5 mg/kg 30 i.v. T1/2 2.31 hr
Dog 3 mg/kg p.o. CL 23.7 mL/min/kg
Dog 5 mg/kg 30 i.v. CL 23.7 mL/min/kg
Mice 1 mg/kg i.v. F 99.0 %
Mice 10 mg/kg p.o. F 99.0 %
Rat 5 mg/kg p.o. F 49.8 %
Rat 5 mg/kg 30 i.v. F 49.8 %
In Vivo

GSK2556286 (0.3-500 mg/kg, p.o, 8 consecutive days) shows greatest effect in acute TB infection mice model receiving 200 mg/kg dosage[2].
GSK2556286 (10-200 mg/kg, p.o., 5 days per week for 4 weeks) shows a significant bactericidal effect in chronic TB infection BALB/c and C3HeB/FeJ mice model, and the maximal effect is achieved with around 10 mg/kg[2].
GSK2556286 (50 mg/kg, p.o., one single dose) has increased efficacy when coadministered with Bedaquiline (B) (HY-14881) (25 mg/kg) and Pretomanid (Pa) (HY-10844) (100 mg/kg) in subacute infection model in BALB/c mice[2].

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

Animal Model: Subacute infection model in BALB/c mice[2]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.)
Result: Resulted in significantly lower lung CFU counts when combined with BPa, BL or BPaL.
Was less active when combined with BL or PaL than BPaL.
Resulted in lower proportions of mice relapsing when combined with BPa or BPaL in comparison with RHZ for 4 months.
Associated with significantly more relapses when combined with PaL, and more relapses after 2 months of treatment when combined with BL.
Clinical Trial
Molecular Weight

329.39

Formula

C18H23N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(CN2CCC(CC2)OC3=CC=CC(C)=C3C)NC(N1)=O
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 : 3.33 mg/mL (10.11 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0359 mL 15.1796 mL 30.3591 mL
5 mM 0.6072 mL 3.0359 mL 6.0718 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0359 mL 15.1796 mL 30.3591 mL 75.8979 mL
5 mM 0.6072 mL 3.0359 mL 6.0718 mL 15.1796 mL
10 mM 0.3036 mL 1.5180 mL 3.0359 mL 7.5898 mL
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GSK2556286 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK25562861210456-20-4GSK286GSK 2556286GSK-2556286GSK 286GSK-286BacterialMycobacterium tuberculosisoral activeantitubercularcholesterol metabolismInhibitorinhibitorinhibit

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