Isoniazid is an antibacterial agent used primarily as a tuberculostatic.Target: AntibacterialIsoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG [1]. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824 [2, 3]. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing [4].

EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.

PSMA-I&T is a PSMA-based radioligand. [177Lu]Lu-PSMA I&T can be uused for potential treatment of metastatic castration-resistant prostate cancer. 67 Ga-PSMA I&T can be used for Radioguided Surgery of Lymph Node Metastases With Biochemical Recurrence of Prostate Cancer

PSMA-BCH also known as NOTA-PSMA, is a PSMA- NOTA-conjugated precursor. 68Ga-PSMA-BCH can be used for prostate cancer imaging. Al18F-PSMA-BCH can be used for prostate cancer imaging as a novel 18F PET radiotracer. 64Cu-PSMA-BCH is a new radiotracer for delayed PET imaging of prostate cancer. 64Cu-PSMA-BCH was PSMA specific and showed high stability in vivo with lower uptake in liver than 64Cu-PSMA-617. Biodistribution in mice and PCa patients showed similar profile compared with other PSMA ligands and it was safe with moderate effective dosimetry.

HYNIC-PSMA is a PSMA based ligand, which can bind radio-active metal ion and used as a tumor-imaging agent in prostate cancer. 99mTc-HYNIC-PSMA is a novel technetium-99m-labeled small-molecule inhibitor of prostate-specific membrane antigen (PSMA) for detection of prostate cancer. 99mTc-HYNIC-PSMA showed high tracer uptake (with a tumor-to-background ratio of 9.42 ± 2.62) in the malignant lesions of PCa patients, making it a promising radiopharmaceutical imaging method for site-specific management of PCa.

WDR5-IN-6 is a WDR5 inhibitor.

Antibacterial agent 133 (4l) is an antimicrobial agent

TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer[1].

PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively[1].

S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor.

PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor

Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor

KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].

LOX-IN-3 Dihydrochloride is an orally active and selective lysyl oxidase (LOX) inhibitor.

GFP16 is a low affinity antiprion compound.

GW6340 is an intestinal-specific LXR agonist.

hCAII-IN-8, an amide, is a highly selective carbonic anhydrase (CA) inhibitor with an IC50 value of 0.18 μM against hCA II[1].

hCAII-IN-9 is a potent carbonic anhydrase inhibitor

CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo[1].

Gcase activator 2 (compound 14), a pyrrolo[2,3-b]pyrazine, is alos a β-Glucocerebrosidase (GCase) activator (EC50=3.8 μM). Gcase activator 2 induces GCase dimerizatio (both K-type and V-type). And Gcase activator 2 has low metabolic clearance in human and mouse[1].

PYZ18 is a selective COX-2 inhibitor with an IC50 of 7.07 μM. PYZ18 is the best lead compound for COX-2 inhibitors. PYZ18 has anti-inflammatory and other biological properties[1].

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity[1].

SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM.

Toluidine Blue is a basic thiazine metachromatic dye with high affinity for acidic tissue components. Toluidine Blue has wide applications in vital staining in living tissues and a special stain.

Cupric sulfate (Copper(II) sulfate) is a salt formed by treating cupric oxide with sulfuric acid. Cupric sulfate is a lewis acid catalyst commonly used to promote acid-catalyzed organic transformations.

TMRM Perchlorate is a cell-permeant cationic lipophilic red fluorescent dye (λex=530 nm, λem=592 nm).

Colestipol hydrochloride, a salt form of Colestipol, is a high-molecular-weight, insoluble, granular copolymer of tetraethylenepentamine and epichlorohydrin. It functions as an anion-exchange and resin-sequestering agent. Colestipol hydrochloride reduces cholesterol levels without affecting triglycerides.

CRCD2 is an NT5C2 (cytosolic 5’ nucleotidase II) inhibitor with a kd of 70.9 μM. It enhances the cytotoxic effects of 6-MP and effectively reverses thiopurine resistance mediated by genetic and non-genetic mechanisms of NT5C2 activation in ALL.

Formamide (Methanamide; Formimidic acid) is a clear liquid amide derived from formic acid. It allows for the denaturation and renaturation of nucleic acids at room temperature. Formamide-induced DNA denaturation when combined with detection of denatured DNA with a monoclonal antibody (MAb) makes it possible to specifically identify the apoptotic cells.