ATB107

Cat. No.: HY-76212: FAQs
Data Sheet SDS Handling Instructions

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

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

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 K_D 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.

455325-51-6

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

Data Sheet (273 KB) SDS (251 KB) Handling Instructions (2659 KB)

References

[1]. Shen H, et al. A novel inhibitor of indole-3-glycerol phosphate synthase with activity against multidrug-resistant Mycobacterium tuberculosis. FEBS J. 2009 Jan;276(1):144-54. [Content Brief]

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	[1]. Shen H, et al. A novel inhibitor of indole-3-glycerol phosphate synthase with activity against multidrug-resistant Mycobacterium tuberculosis. FEBS J. 2009 Jan;276(1):144-54. [Content Brief]

ATB107 Related Classifications

Infection

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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.

Keywords:

ATB107455325-51-6ATB 107ATB-107OthersInhibitorinhibitorinhibit

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