T6049

SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.

Melatonin receptor agonist 1 (compound 20c) is a potent agonist of the melatonin receptor (MT) with Ki values of 108 nM for MT2 and 1140 nM for MT1 [1].

Elongation factor P-IN-1, a potent elongation factor P (EFP) inhibitor and β-lysine derivative compound, affects E. coli proliferation rate[1].

Lamotrigine hydrate is an effective oral active anticonvulsant or antiepileptic agent that selectively blocks voltage-gated Na + channels, stabilizes presynaptic neuronal membranes and inhibits glutamate release. Lamotrigine hydrate can be used in epilepsy, focal seizure, et al [1] [2].

Metallo-β-lactamase-IN-7 is a potent inhibitor of VIM-type metallo-β-lactamase with IC50 values of 0.019 μM, 13.64 μM, and 0.38 μM for VIM-2, VIM-1, and VIM-5, respectively. Metallo-β-lactamase-IN-7 also enhances the antibacterial activity of Meropenem against Gram-negative bacterial strains [1].

PARP10/15-IN-1 (compound 8l) is a dual inhibitor of PARP10 and PARP15, with IC50 values of 160 nM and 370 nM, respectively. It is applicable in cancer research[1].

Ketorolac (RS37619) hemicalcium is a nonselective COX inhibitor with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This non-steroidal anti-inflammatory drug (NSAID) is used as a 0.5% ophthalmic solution for researching allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, it is a DDX3 inhibitor applicable in cancer research [1] [4].

MRGPRX1 agonist 3 (compound 1f) is a potent positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MRGPRX1) with an EC50 of 0.22 μM, and it can be used for neuropathic pain research[1].

Chlorpheniramine is an H1 anti-histamine agent for IgE-mediated inflammation that is commonly used for allergic diseases.

IDO1/TDO-IN-2 (Compound 1) is a potent dual inhibitor of IDO1 and TDO with IC50 values of 0.1 μM and 0.07 μM, respectively. It holds potential for cancer research[1].