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

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.

SSR125543 (Crinecerfont, SSR-125543) is a potent, nonpeptide, orally active corticotropin-releasing factor (CRF) receptor CRF1 antagonist, shows anxiolytic- and antidepressant-like activities in vivo. .

GLP-1(7-36), amide is a physiological incretin hormone that stimulates insulin secretion.

Ensartinib, also known as X-396, is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development.

Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.

A potent inhibitor of tumor promoting phorbol ester TPA/PMA and inhibitor of Ca2+/calmodulin dependent EF-2 phosphorylation

Amastatin HCl is an aminopeptidase inhibitor that also induces vasoconstriction.

Phenylacetylglutamine is used as biomarker for metabolic age.

ER-464195-01 is a specific, orally active inhibitor that inhibits Calreticulin (CRT) binding to integrin α subunits (ITGAs) with IC50 of 0.17, 0.36, and 0.23 uM in the interaction between CRT and ITGA α4, αL, and αM/α2/α5.

AGF347 (AGF-347) is a small molecule inhibitor targeting mitochondrial C1 metabolism at SHMT2 (in vitro Ki=2.19 uM), also directly targers the purine biosynthetic enzymes GARFTase (Ki=3.13 uM) and AICARFTase (Ki=3.72 uM), and SHMT1 (Ki=2.91 uM).

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 2.8 uM, inhibits the phosphorylation of OAG to OAPA with IC50 of 3.8 uM in intact platelets.

LBL1 is a first-in-class pyrroloquinazoline small molecule that selectively targets the coiled-coil domain of lamin A (binding affinity Kd = 5.11 μM), demonstrating potent anticancer effects through nuclear lamina disruption.

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

WQ-2101 (WQ2101, PKUMDL-WQ-2101) is a specific, allosteric inhibitor of PHGDH with IC50 of 34.8 uM (WT PHGDH), shows dramatically reduced potenecy for mutants R134A (IC50 =141 uM) and K57AT59A (IC50=128 uM).

ZLD1039 is a novel, orally active EZH2 inhibitor demonstrating high selectivity and potency. It effectively suppresses PRC2 enzymatic activity across wild-type EZH2 (IC50 = 5.6 nM) and mutant forms (Y641F: 15 nM; A677G: 4.0 nM), while exhibiting significant anti-tumor and anti-metastatic effects in breast cancer models.

LY305 is a potent non-steroidal SARM exhibiting high androgen receptor binding affinity (Ki = 2.03 nM) and strong agonist activity in C2C12 cells (EC50 = 0.499 nM), demonstrating its selective modulation capabilities.

NNK is a procarcinogen, a major tobacco-specific toxicant that inhibits the expression of lysyl oxidase, a tumor suppressor.

VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.

Tradipitant (VLY-686) is a selective neurokinin-1 (NK-1) receptor antagonist with potential therapeutic applications.

SKI-178 is a potent, specific, non-lipid SphK1 inhibitor with Ki of 1.33 uM, displays no significant activity for SphK2 (IC50>25 uM).

SW-100 (SW100) is a potent, selective, brain penetrable HDAC6 inhibitor with IC50 of 2.3 nM, displays >1,000-fold selectivity over all other class I, II, and IV HDAC isoforms.