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Molecule- SPK-HD-14

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Molecule- SPK-HD-14

SPK-HD-77

SPK-HD-14 is a highly potent and novel IMPDH inhibitor for the species Helicobacter pylori, shown to exhibit nanomolar range of enzyme inhibition through in vitro assays. The biochemical studies of SPK-HD-14 reveal its uncompetitive mode of inhibition on H. pylori IMPDH (HpIMPDH) with an IC50 value of 0.095 ± 0.023 μM1 and high specificity over human IMPDH II.

Purity: > 99% (HPLC)

Biological activity:

1. SPK-HD-14 is a highly potent and novel HpIMPDH inhibitor with an IC50 value of 0.095 ± 0.023 μM, determined using in-house developed in vitro enzyme inhibition assays.
2. Kinetic characterization of SPK-HD-14 on HpIMPDH reveals that the molecule inhibits the enzyme mechanism with using uncompetitive inhibition.
3. SPK-HD-14 shows approximately 1.5×103-fold increase in selectivity towards HpIMPDH over human IMPDH II, making it a suitable drug-like molecule.1

Physicochemical Properties:

Molecular Weight365.8210
FormulaC19H16ClN5O
AppearanceWhite solid powder
Storage

Solid powder

-20°C 12 Months; 4°C 6 Months

In Solvent

-80°C 6 Months; -20°C 6 Months

Solubility10 mM in DMSO

References:

(1)Dilip, H.; Thiruvenkatam, V.; Kirubakaran, S. Studies on Methylpyrazole-Substituted Benzimidazoles to Target Helicobacter Pylori Infection through HpIMPDH Inhibition. ACS Infect. Dis. 2024. https://doi.org/10.1021/acsinfecdis.4c00228.

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