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ATB107 is a novel and potent inhibitor of indole-3-glycerol phosphate synthase (IGPS) with a KD of 3 μM.

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

ATB107 Chemical Structure

ATB107 Chemical Structure

CAS No. : 455325-51-6

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Description

ATB107 is a novel and potent inhibitor of indole-3-glycerol phosphate synthase (IGPS) with a KD of 3 μM.

IC50 & Target

KD: 3 μM (IGPS)[1]

In Vitro

The minimum inhibitory concentration (MIC) of ATB107 is 0.1 μg/mL for M. tuberculosis H37Ra. ATB107 also has high activity against M. tuberculosis H37Rv, with an MIC of 0.1 μg/mL. All 50 fully susceptible clinical isolates tested are susceptible to ATB107 at 1 μg/mL; of these, 41 (82%) are susceptible to ATB107 at 0.1 μg/mL. The results also show that 67 (83.8%) multidrug-resistant TB (MDR-TB) isolates are susceptible to ATB107 at 1 μg/mL, and 25 (31.3%) isolates are susceptible to ATB107 at 0.1 μg/mL. Results show that the binding ability of ATB107 is well correlated with its concentrations. At the highest concentration of 200 μg/mL, ATB107 can inhibit cell proliferation, with cell survival of about 60%. With the lower concentration of 50 μg/mL, cell survival is more than 80% for ATB107[1].

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

Molecular Weight

392.50

Formula

C21H28N8

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

C1(N2CCCCC2)=NC(NC3=CC=CC=C3)=NC(N/N=C4CN5CCC\4CC5)=N1

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
Purity & Documentation
References
Kinase Assay
[1]

The concentration of mIGPS is determined. The substrate CdRP is chemically synthesized, with a yield of 30 mM. Ten microliters of 30 mM CdRP and 10 μL of 1.24 μM IGPS are added to 480 μL of 5 mM Tris/HCl (pH 7.0), and incubated at 37°C for 20 min. The enzyme activity is measured with a spectrophotometer by following the increase in absorbance of the solution at 280 nm. ATB107 is added to the assay mixture to obtain concentrations of 10-4 M, 7.5×10-5 M, 5×10-5 M, 2.5×10-5 M, and 10-5 M, respectively[1].

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

Cell Assay
[1]

The tetrazolium dye reduction assay [3-[4,5-dim-ethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT)] is used to determine the effect of ATB107 on cell survival and growth. At first, the THP-1 macrophage cells are inoculated at 8×104 cells/mL) into 96-well plates and incubated at 37°C in a 5% CO2/95% air atmosphere for 24 h. ATB107 is added to give concentrations of 50,100, 150 and 200 μg/mL. After incubation of cells treated with ATB107 for 12 h, 20 μL (5 g/L) of MTT solution is added to each well; this is followed by incubation for another 4 h to allow the formation of formazan crystals. Finally, 10% SDS is added to dissolve the formazan crystals, and the plates are read on a microplate reader at 570 nm. Controls are included in which only culture media are added to wells containing cells[1].

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

References
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ATB107 Related Classifications

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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.

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Product Name:
ATB107
Cat. No.:
HY-76212
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