CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.

Novel selective c-Myc inhibitorReference:1) Disruption of Myc-Max heterodimerization with improved cell-penetrating analogs of the small molecule 10074-G5; Oncotarget. 2013 Jun;4(6):936-47. GoTo Paper

Tamibarotene(Am-80) is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.

ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.

Mirk-IN-1 is a potent, specific inhibitor of Dyrk1B (Mirk kianse) and Dyrk1A with IC50 of 68 nM and 22 nM respectively, shows SW620 cell IC50 of 1.9 uM.

INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.

EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

GAC0003A4 is an LXR inverse agonist that inhibits LXR transcriptional activity. GAC0003A4 also efficiently degrades LXRβ protein. GAC0003A4 has the potential to be used in advanced pancreatic cancer and other refractory malignancies.

EN460 is a specific mall molecule inhibitor of endoplasmic reticulum oxidation 1 (ERO1), interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation (IC50=1.9 uM).

SCH 529074 is a small molecule mutant p53 reactivator that binds p53 DNA binding domain with Kd of 1-2 uM.

Merck60 (BRD 6929, Compound-60) is a potent, selective and brain-penetrant inhibitor of HDAC1 and HDAC2 with IC50 of 1 nM and 8 nM respectively.

A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM.

Aspalatone is an anti-platelet aggregator (antithrombotic) that has been shown to prolong bleeding time in the mouse model. Aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy.

(E/Z)-CCR-11 (Comp 12) is a selective CD38 inhibitor, with an IC50 of 20.8 μM against CD38 cyclase. (E/Z)-CCR-11 promotes increases in cellular NAD+ levels and interferon γ.

Novel inhibitor of PKM2-regulated signaling, suppressing non-glycolytic PKM2-regulated signaling in cancer cells

Ameltolide, a 4-aminobenzamide derivative, is an anticonvulsant agent which has been shown to be effective at inhibiting seizures in animal models.

Novel LXR inverse agonist, functioning as LXR a degrader, significantly reducing LXR protein levels in PDAC cell lines

LUF7346 is a novel hERG allosteric modulator that slows IKr deactivation and positively shifting IKr inactivation.

VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity.

Dual dopamine D2 and muscarinic M1 receptor ligand with putative antipsychotic and pro-cognitive potential

VU0366248 is a mGlu5 negative allosteric modulator.

Cl-amidine (hydrochloride) is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells.

CCCI-01 is an inhibitor of centrosome clustering in cancer cells.

Chlorfenson is used to treat onychomycosis (nail fungus) as the primary indication.

Novel highly-selective melanocortin-4 receptor (MC4R) agonist, increasing resting energy expenditure in obese individuals

Novel potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor

A small molecule tumor translocation inhibitor that inhibits the prostate cancer cell transcriptional program, in part by inhibition of the demethylase KDM4C (IC50=30 uM).

Novel 37/67kDa laminin receptor (LR) inhibitor, affecting both the direct 37/67kDa LR-PrP(C) interaction in vitro and the formation of the immunocomplex in live cells, inducing a progressive internalization of 37/67kDa LR and stabilization of PrP(C) on th