AOH1996 is a proliferating cell nuclear antigen (PCNA) inhibitor. AOH1996 enhances PCNA and RPB1 interaction and interferes with TRC resolution and induces DNA double-stranded breaks in a transcription dependent manner. AOH1996 almost completely inhibits the growth of xenograft tumors without causing any discernible toxicity to experimental animals.AOH1996 has superior metabolic stability as compared to the AOH1160 parent molecule. 

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.