t-12

VBIT-12 is a potent inhibitor of VDAC1.

BMT-124110 is a selective AAK1 inhibitor (IC50: 0.9 nM) with antinociceptive activity. BMT-090605 inhibited BMP-2 induced protein kinase BIKE with IC50 of 17 nM. BMT-090605 inhibits cyclin G-associated kinase GAK with an IC50 of 99 nM.

BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.

PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

AT-121 hydrochloride is a dual agonist of nociception and mu opioid receptor with Ki values of 3.67 and 16.49 nM, respectively.AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity. AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity.

(Iso)-BMT-124110 Formate has an inhibitory effect on the protein serine threonine kinase AAK, and is used in the treatment of Parkinson's disease, schizophrenia, neuropathic pain, and Alzheimer's disease.

Antileishmanial agent-12 (compound 5a) is a potent antileishmanial agent with antibacterial activity against Leishmania braziliensis (IC50: 14.9 μM), Leishmania infantum (IC50: 21.3 μM), and T. cruzi (IC50: 9.3 μM), demonstrating significant antiprotozoal effects.

PAT-1251 Hydrochloride is a potent, selective, and oral inhibitor of lysyl oxidase-like 2 (LOXL2), targeting hLOXL2 and hLOXL3 with IC50 values of 0.71 and 1.17 μM, respectively.

Antituberculosis agent-12 (compound 3408) is a narrow-spectrum prodrug of a phosphate, designed to inhibit resistant tuberculosis infections.

Antibiofilm agent-12 (Compound C13), an antifungal belonging to the carbamate derivatives, exhibits significant antifungal activity against Candida auris, with an MIC90 of 237.9 μM. It inhibits the drug efflux pump activity of Candida auris and promotes ergosterol depletion, thereby hindering the formation of Candida auris biofilms and reducing its metabolic flexibility. Additionally, Antibiofilm agent-12 demonstrates antifungal efficacy in a C. elegans model following Candida auris infection.

CFT-1297 is a BET PROTAC degrader that targets BRD4 for degradation.

PT-129 is a RPOTAC degrader that targets the G3BP1 2NTF2 domain (protein-RNA interaction site), facilitating the breakdown of intracellular stress granules. It prevents the formation of stress granules in stressed cells and deconstructs existing ones, thereby disrupting ATF4 transmission and inhibiting cancer cell proliferation. Stress granules (SGs) are membraneless cytoplasmic compartments formed under stress, which aid in the transfer of ATF4 from fibroblasts to tumor cells, promoting fibroblast-related tumor growth. G3BP1 2 serve as central proteins in the SG network, and inhibiting them may reduce the stress resilience of cancer cells within the tumor microenvironment. PT-129 consists of a target protein ligand (red part) G3BP1 2-Targeting ligand-1, an E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a PROTAC linker (black part) Amino-PEG3-C2-acid; the E3 ligase ligand and linker form the complex Thalidomide-NH-PEG3-propionic acid.

KNT-127 is an agonist of δ-Opioid receptor.

Zt-12-037-01 is a ATP competitive STK19 inhibitor(IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N),respectively).

Antitubercular agent-12 (Compound 2c) is a highly effective antitubercular agent with a MIC (Minimum Inhibitory Concentration) value of 1.439 μg mL and significantly reduced cytotoxicity, evidenced by a CC50 (50% Cytotoxic Concentration) value of 57.34 μg mL [1].

ZLMT-12 (compound 35) is a tacrine derivative and a potent inhibitor of CDK2 (IC50: 0.011 μM) and CDK9 (IC50: 0.002 μM). ZLMT-12 weakly inhibits AChE (IC50: 19.023 μM) and BuChE (IC50: 2.768 μM). ZLMT-12 has anti-proliferative activity and low cytotoxicity. ZLMT-12 blocks the cell cycle in S-phase and G2 M-phase and induces apoptosis.

FHT-1204 is a potent inhibitor of SMARCA4 SMARCA2 ATPase (BRG1 and BRM) (IC50 ≤ 10 nM).

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

Antiproliferative Agent-10 (Compound 1), a ruthenium(II)-tris-pyrazolylmethane complex, functions as an anti-tumor agent by impeding cancer cell proliferation through the inhibition of mitochondrial calcium uptake [1].

Antimicrobial agent-12 serves as a powerful antibacterial compound that also exhibits inhibitory activity against SARS-CoV-2 [1].

Antitumor agent-120 (compound 1), a flavonoid derived from Kudzu root, exhibits negligible inhibitory effects on LNCaP and PC3 cancer cells, with IC50 values exceeding 50 μM [1].

Antitumor Agent-122 (Compound 5j), characterized by its effective antitumor properties and minimal toxicity and resistance, exhibits strong antiproliferative effects against various cancer cell lines, including MGC-803, HepG2, SKOV3, and T24. It demonstrates IC 50 values of 5.23 μM, 3.60 μM, 1.43 μM, and 3.03 μM, respectively [1].

Antitumor agent-128 (compound 1a) induces cell cycle arrest in the G2 M and S phases, leading to apoptosis in A549 cells [1].