5,5-Diphenylbarbituric acid is an organic compound belonging to the derivatives of barbituric acid. 5,5-Diphenylbarbituric acid can be used for seizure study.

4F-Docetaxel (4FDT) is a fluorinated docetaxel analog. 4F-Docetaxel has anti-hepatoma activity and can be used for research of hepatocellular carcinoma (HCC).

A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.

AM 432 is potent, selective, orally active prostaglandin D2 receptor (DP2/CRTH2) antagonist with binding IC50 of 6 nM for hDP2.AM-432 shows no cross-reactivity against the TP or IP receptors, COX-1 or COX-2 and minimal activity at DP1 receptor. AM432 shows excellent potency in a human whole blood eosinophil shape change assay.AM432 exhibits efficacy in both a murine model of allergic rhinitis and a cigarette smoke induced inflammatory model of COPD.

Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.

Novel Inhibitor of TonB Function

A potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2, ACAT2) with IC50 of 11.8 nM, >6,000-fold selectivity over ACAT1.

A derivative of the antifungal drug itraconazole (ITA) as an inhibitor of MFB cell fate in resident fibroblasts derived from multiple murine and human tissues.

RS-0406 is a novel beta-sheet breaker, RS-0406 reverses amyloid beta-induced cytotoxicity and impairment of long-term potentiation in vitro. RS-0406 arrests amyloid-beta oligomer-induced behavioural deterioration in vivo.

HTS13286 is a selective AQP9 inhibitor with IC50 of 1.5 uM (inhibition of CHO-AQP9 cell water permeability).

2-Amino-2-deoxyglucose hydrochloride is a hexosamine hydrochloride can be used in the synthesis of cyclopropene-modified hexosamine derivative Ac4GlcNCyoc and Ac4GalNCyoc.

PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.

PSMA617-TCMC is a derivative of PSMA-617 with structure modification, in which the caroboxy groups in DOTA ring is replaced by TCMC macrocycle. PSMA-617 is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer,. PSMA-617 originally was developed at the German Cancer Research Center and the Heidelberg University Hospital. ABX held the exclusive license to bring the treatment, which targets prostate-specific membrane antigen (PSMA), through early clinical development.

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

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

Lomeguatrib (PaTrin-2) is a modified guanine base, which can repress the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) with an IC50 value of 6 nM.

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

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.

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).

DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96).

Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.

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

TBA-7371 (TBA7371, AZ 7371) is a potent, non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) with IC50 of 10 nM, an enzyme involved in mycobacterial cell wall biogenesis.TBA-7371 also inhibits PDE6 with an IC50 value of 4 uM.TBA-7371 is active against M. tuberculosis with an MIC range of 0.78-3.12 µM and demonstrates efficacy in a rodent model of tuberculosis.

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.

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.

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

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

Mafodotin, also known as mc-MMAF and SGD-1269 or Maleimidocaproyl monomethylauristatin F, is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful a

IC8 is an ionizable cationic lipid. It has been used in combination with other lipids for the formation of lipid nanoparticles (LNPs). Immunization with severe acute respiratory coronavirus 2 (SARS-CoV-2) spike glycoprotein mRNA in IC8- and manganese-containing LNPs induces IgG responses to SARS-CoV-2 Delta and Omicron variants in mice.1 Administration of mRNA encoding B7-H3 X CD3 bispecific T cell engaging (BiTE) antibodies in IC8-containing LNPs reduces tumor growth in MV4-11 and A375 mouse xenograft models.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.