GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

Prinomastat (AG3340) is a potent, selective MMP inhibitor with pM affinities for inhibiting gelatinases (MMP-2 and -9, Ki=50-150 pM), MMP-14 and MMP-13; demonstrates broad antitumor activity in a number of tumor models, inhibits glioma invasion or growth of the human malignant glioma cell line U87; also suppresses tumor growth in a malignant glioma tumor model.

Atabecestat (JNJ-54861911, JNJ54861911) is a novel potent, oral beta-secretase (BACE) inhibitor for treatment of Alzheimer's Disease.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.

AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.

Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances. PGD2 plays a protective role by suppressing inflammation.

TDI-11861 is second-generation soluble Adenylyl Cyclase (sAC, ADCY10) inhibitor with slow dissociation rates. TDI-11861 inhibits sAC cellular with an IC50 value of 5.5 nM.

Dnp-PLG-Cys(Me)-HA-DArg-NH2 is a peptide substrate for matrix metalloproteinase-1 (MMP-1).It has an improved kcat/Km ratio compared with the MMP-1 flurogenic substrate Dnp-PLGLWA-DArg-NH2.

MMP-3 inhibitor is a peptide inhibitor of matrix metalloproteinase-3 (MMP-3) with a Ki value of 95 nM.

Ribavirin carboxylic acid (TR-COOH) is a metabolite of ribavirin, ribavirin has strong antiviral activity.

BVT 14225 is a new selective 11b-HSD1 inhibitor, it belongs to a class of arylsulfonamidothiazoles with in vitro and in vivo antidiabetic effects

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.

BMS-986205 is an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic activity, alone and in combination with nivolumab in advanced cancers in a phase 1/2a trial

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.

Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.

Dnp-PLAYWAR is a fluorogenic substrate for matrix metalloproteinase-8 (MMP-8) and MMP-26.The activity of MMP-8 and MMP-26 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitro

Dnp-P-Cha-G-Cys(Me)-HA-K(Nma)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-9

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.

OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study.

ACT001(DMAMCL, dimethylaminomicheliolide) is a PAI-1 inhibitor and exerts antitumor effects on neuroblastoma (NB) both in vitro and in vivo. It also exerts synergistic effects in combination with cisplatin through the inhibition of the PAI-1/PI3K/AKT pathway.

Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.

(R)-SW203668 (SCD inhibitor (R)-27) is a potent, tumor-specific, irreversible stearoyl CoA desaturase (SCD) inhibitor with high sensitity to H2122 cell (IC50=11 nM).

Sanofi-14h is a selective inhibitor of the AGC family kinase SGK3, blocks DMXAA-stimulated IRF3-promoter activity with IC50 of 1.73 uM, inhibits IFNβ production under STING stimulation.

SBI-668 is a selective inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM in isothermal CETSA assays, 7-fold selectivity over SHP2-WT (IC50=15 uM).

SBI-221 is a small molecule inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM and 7.4 uM for SHP2-E76K and SHP2-WT in isothermal CETSA assays, respectively.

NSC49L (NSC30049) is a small molecule agonist (activator) of protein phosphatase 2A (PP2A), specifically stimulates PP2A-Cα activity with Kact of 14 nM, downregulates the AKT1/mTOR/4EBP1-axis, and inhibits p21 translation.