PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.

The major circulating metabolite of vitamin D3.

NecroX-5 is a novel necroptosis inhibitor that reduces mitochondrial oxidative stress, prevents hypoxia/reoxygenation injury by inhibiting the mitochondrial calcium uniporter.

Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

Gadodiamide is a gadolinium-based contrast agent used in MR imaging procedures to assist in the visualization of blood vessels. Target: OthersGadodiamide(Omniscan) is a gadolinium-based contrast agent used in MR imaging procedures to assist in the visualization of blood vessels. Gadodiamide is a contrast medium for cranial and spinal magnetic resonance imaging (MRI) and for general MRI of the body after intravenous administration. The product provides contrast enhancement and facilitates visualisation of abnormal structures or lesions in various parts of the body including the central nervous system (CNS). A recent review takes the question of toxicity caused by loss of gadolinium from the complex. "The challenge for nephrologists includes (a) evidence of transmetallation, such as gadolinium deposits in bone, increased urinary zinc excretion, iron-transferrin dissociation or 'spurious hypocalcemia' in exposed people"。

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

GS-7340(Tenofovir alafenamide) is a prodrug of tenofovir (TFV) that more efficiently delivers TFV into lymphoid cells and tissues than TFV disoproxil fumarate.

Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.

2'3'-cGAMP has been used to identify small compounds capable of binding human stimulator of interferon genes (STING). It is also used to study type I interferon response to cytosolic DNA.

Gentamycin sulfate (Gentacycol)

IMP-1710 (IMP1710) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 38 nM.IMP-1710 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.IMP-1710 can profile activity of endogenous UCHL1 with excellent selectivity in cell types including endothelial cells (EA.hy926) and adenocarcinoma human alveolar basal epithelial cells (A549).IMP-1710 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=740 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.IMP-1710 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.

KB-R7943 mesylate is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 mM).

An aminoglycoside antibiotic similar in structure to gentamicin B1.

Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).

Tematropium(CDDD3602) is a soft anticholinergics.

1-Methoxy PMS is an electron mediator for NAD(P)H-tetrazolium salt.

Micafungin(FK463) is an echinocandin antifungal drug, Micafungin inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls.

Avibactam sodium(NXL-104) is a non-β-lactam β-lactamase inhibitor antibiotic.

UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6.

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.

L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.

Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.

DS-437 is a potent, selective, dual inhibitor of PRMT5 and PRMT7 with IC50 of 6.0 uM for both, DS-437 is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases.

TL 13-27 is a negative control for TL 12-186. Demonstrates no kinase degradation in vitro.

Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.