Immethridine (hydrobromide) is a histamine agonist selective for the H3 subtype.

DMPQ dihydrochloride is a potent and selective inhibitor of human platelet-derived growth factor receptor β (PDGFRβ) with an IC50 of 80 nM.

NAV 26 (compound 26) is a selective voltage-gated sodium channel Nav1.7 blocker with an IC50 of 0.37 μM. NAV 26 can be used for pain research.

rac-NBI-74330 is a potent and selective CXCR3 antagonist.

SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.

ML 339 is a potent and selective hCXCR6 antagonist (IC50 = 140 nM), 100-fold less active at the murine CXCR6 receptor (IC50 = 18 uM); ML 339 exhibits selectivity over CXCR5, CXCR4, CCR6 and APJ receptors.

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.

LUF6283 is a partial agonist of hydroxycarboxylic acid receptor 2

2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).

Prodrug of INDY, a novel potent ATP-competitive Dyrk1A inhibitor

A-350619 hydrochloride is an activator of soluble guanylyl cyclase (sGC).

CYM-5478 is a potent, selective agonist for S1P2. Under nutrient-deprivation stress produced by serum-starvation, CYM-5478 induced a statistically significant increase in the viability of C6 cells in a dose dependent manner at concentrations above 100?nM.

Novel inhibitor of chromosomal instability, potentiating MCAK in vivo and transiently suppressing chromosome mis-segregation in CIN cancer cells

Novel FAK activator, promoting human intestinal epithelial monolayer wound closure and mouse ulcer healing

PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect.

inh-02 (RNF5 inhibitor inh-02) is a novel small molecule inhibitor of E3 ubiquitin ligase RNF5/RMA1.

GW-8510 (GW8510) is a potent, selective inhibitor of CDK2 with IC50 of 10 nM.

SR 16584 is a selective antagonist of α3β4 nAChR with an IC50 of 10.2 μM.

ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.

A potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a..

Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).

mG2N001 is a potent negative allosteric modulator (NAM) of metabotropic glutamate receptor 2 (mGluR2) with IC50 of 93 nM.

INR119 is a small molecule allosteric MAPKK (MAP2K, MEK1/2) inhibitor, binds fission yeast homologue Wis1 near C458 and protects Wis1 from inactivation by low levels of H2O2 in vitro.INR119 pretreatment strongly potentiates the Wis1 response to low H2O2 in vivo.Phosphorylation of Sty1 depends entirely on activated Wis1, and the INR119-induced enhancement of Sty1 pathway activation upon H2O2 stress requires the upstream activation of Wis1 through the MAPKKKs.

VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.

Potent and specific pan-PIM inhibitor, inhibiting proliferation of several AML cell lines, showing dual antitumoral and bone antiresorptive effects

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).

MGH-CP1 is a potent and selective TEAD palmitoylation inhibitor.

iBAP (BAP1 inhibitor I) is a first-in-class inhibitor of the catalytic activity of BAP1 histone H2A deubiquitinase complex with IC50 of 0.5-1 uM in vitro,

iBAP-II (BAP1 inhibitor II) is a next-generation, specific small molecule inhibitor of BAP1 histone H2A deubiquitinase activity with IC50 of <0.1 ug/mL.iBAP-II displays higher affinity for BAP1 than the closest UCH family member, UCHL5, and other deubiquitinases, such as USP5, USP7, USP8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3.Inhibition of BAP1 via iBAP-II reduces ASXL3 protein stability in small cell lung cancer cells, without significant changes to ASXL1 and ASXL2 protein levels.iBAP-II suppresses ASCL1 expression in NCI-H1963 cells, along with the mRNA levels involving a handful of known ASCL1 transcriptional targeted genes, such as GRP, DMPK, RNF183, SCN3A, MYCL, and CACNA1A.iBAP-II exhibited more potent cell viability inhibition activity on four different BAP1-WT SCLC cell lines than iBAP.iBAP-II (50 mg/kg/d) significantly delayed the disease progression in SCLC xenograft model.

F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.