ICT12035 (AZ2158) is a potent, selective formylpeptide receptor-1 (FPR1) antagonist with IC50 of 30 nM in calcium mobilisation assays (100 nM fMLF).

Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.

SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM).

6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.

HL-43 (EP4 antagonist HL-43) is a selective prostaglandin E receptor 4 (EP4) antagonist, promotes chondrocyte differentiation/cartilage regeneration and anabolism with low toxicity; HL-43 exhibits the highest potency in inducing Col2a1 expression and reducing Mmp3 expression in presence of IL-1β. HL-43 downregulats Mmp3/13 expression in a dose-dependent manner. HL-43 induces anabolic factors (ACAN and SOX9), and suppresses catabolic factor (MMP13), and hypertrophic marker (COLX), inhibits the STAT3 catabolic pathway;. HL-43 promotes chondrocyte differentiation and ECM generation, and inhibits matrix degradation in both human and mouse articular cartilage explants. HL-43 enhances cartilage repair and regeneration in different artilage defect (CD) animal models.

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

CW5107 (CW 5107) is a small molecule HSD17B7 inhibitor that enhances oligodendrocyte formation.

Benzocaine hydrochloride is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

Tavapadon is a potent, orally-bioavailable, selective partial agonist of the dopamine D1 and D5 receptors.

TFAX 488,SE dilithium, an amine reactive green fluorescent dye, is insensitive to pH in the range 4-10. TFAX 488,SE dilithium forms bright and photostable conjugates with proteins and antibodies. TFAX 488,SE dilithium is suitable for use in flow cytometry, two-photon excitation microscopy (TPE), and super resolution microscopy techniques, such as dSTORM, SIM and STED. Excitation maximum=495 nm; emission maximum=515 nm; extinction coefficient=73,000 M-1cm-1; quantum yield=0.92.

Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases.

GTP-14564 is a specific kinase inhibitor for ITD-FLT3. GTP-14564 inhibited the growth of interleukin-3-independent Ba/F3 expressing ITD-FLT3 at 1 microM, whereas a 30-fold higher concentration of GTP-14564 was required to inhibit FLT3 ligand-dependent growth of Ba/F3 expressing wild type FLT3 (wt-FLT3).

Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.

TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes.

FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).

A293 (AVE1231) is a potent and antiarrhythmic compound and selective inhibitor of two-pore-domain potassium channel TASK-1 (KCNK3, hK2P3.1).A293 (AVE1231) is an inhibitor of hKv1.5 currents with predominant action on channels in their open state.A293 (1 uM) prominently depolarized arterial smooth muscle and increased basal tone level and contractile responses to methoxamine of arteries from young rats but had almost no effect in adult rats.Pharmacological inhibition of atrial TASK-1 currents via A293 (AVE1231) exerts antiarrhythmic effects in vivo as well as in silico, resulting in acute cardioversion of paroxysmal trial fibrillation (AF).

BDM44768 (BDM 44768) is a potent, selective catalytic site inhibitor of insulin-degrading enzyme (IDE) with IC50 of 60 nM (hIDE). BDM44768 displays excellent selectivity over a panel of metalloproteases (>45-fold selectivity over hNEP and hECE, no significant acitivity against hACE and hMMP-1). BDM44768 significantly increased concentrations of Aβ1-40 in culture supernatants of human SY5Y neuroblastoma cells. Acute treatment of mice with BDM44768 (50 mg/kg, i.p.) increases insulin signalling and surprisingly impairs glucose tolerance in an IDE-dependent manner in C57BL/6J mice.

GLPG2451 (GLPG 2451) is a potent potentiator of cystic fibrosis transmembrane conductance regulator (CFTR) with EC50 of 11 nM for F508del CFTR in the YHA assay and EC50 of 18 nM in TECC assay using HBE cells from patients carrying the F508del mutation. GLPG2451 improves the gating function of the CFTR channel.

MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.

SB699551 is a potent, selective 5-HT5A receptor antagonist with pKi of 8.3, >100-fold selectivity over 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors. SB699551 also is a novel PSMD4/Rpn10 inhibitor, decreases cell viability in MM cell lines.

Vidofludimus (IMU-838) is a selective and potent second-generation dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 160 nM, shows anti-SARS-CoV-2 activity with EC50 of 7.6 uM in Vero cells. Vidofludimus inhibits T cell proliferation with EC50 of 11.8 uM, with a similar effect on CpG ODN 2006-PTO dependent B cell proliferation. Vidofludimus is specific for human DHODH and does not have off-target effect on kinases, is about 7.5-fold and about 64.4-fold more active on human DHODH as compared to rat DHODH and mouse DHODH, respectively. Vidofludimus inhibits specifically IL–17F, IL–17A and IFN-g expression in PBMCs. Vidofludimus is 2.6 times more potent in inhibiting DHO oxidation by human DHODH compared to teriflunomide (IC50=420 nM). Vidofludimus shows inhibition of rat EAE motor signs in a rat experimental autoimmune encephalomyelitis (EAE) model. Vidofludimus exerts a broad-spectrum activity against a selection of major human pathogenic viruses.

BDM88951 (BDM 88951) is a highly potent, selective inhibitor of endoplasmic reticulum aminopeptidase 2 (ERAP2) with IC50 of 19 nM. BDM88951 displays selectivity index (>150) towards closely related ERAP1 and IRAP enzymes, as well as MMPs, TACE and LAP3. BDM88951 is a potent inhibitor of ERAP2-mediated hydrolysis of two nonapeptides precursors of SIINFEKL, an ovalbumine-derived antigen, in a dose dependent manner. BDM88951 engage ERAP2 in cells and inhibits antigen presentation in a cellular context, also displays favorable in vitro ADME properties and in vivo exposure.

FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms.

Zastaprazan is a proton pump inhibitor (WO2018008929). Zastaprazan can be used for the research of gastrointestinal inflammatory diseases or gastric acid-related diseases.

O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

MO-I-1182 is a small molecule inhibitor of aspartate beta-hydroxylase (ASPH), suppresses cholangiocarcinoma metastasis.

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.

RBF197 (RBF-197) is a novel highly potent and selective eIF4A inhibitor, inhibits human eIF4A helicase activity with IC50 of 55.2 pM.