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.

Novel agonist of the water channel aquaporin-1 (AQP1)

JXL069 is a novel mitochondrial pyruvate carrier (MPC) inhibitor being investigated for its therapeutic potential in treating alopecia and hair growth disorders.

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

ProSeAM is a chemical tool for methylome analysis.

FTT5 is a lipid-like compound for efficient delivery of long mRNAs in vivo.

CLinDMA, a cationic lipid known to potentially trigger inflammatory responses, is utilized in the synthesis of LNP201. This liposome-based assembly is specifically designed for the systemic delivery of siRNA.

DOIC is a cationic lipid that can be used for RNA vaccines.

UHMCP1 is a small molecule that prevents the SF3b155/U2AF65 interaction, binds to the hydrophobic pocket of the U2AF65 UHM domain (Kd=1-20 uM), impacts splicing and cell viability.

Novel pendrin inhibitor, inhibiting Cl-/anion exchange mediated by mouse pendrin without affecting other major kidney tubule transporters

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).

2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0.

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.

SD-36 (STAT3 degrader SD-36) is a potent, selective STAT3 degrader (PROTAC), potently induces the degradation of STAT3 protein in vitro and in vivo.SD-36 is designed using an analogue of CRBN ligand lenalidomide and the STAT3 inhibitor SI-109, binds to recombinant STAT3 protein with Ki of 11 nM.SD-36 (250 nM) depleted >90% of STAT3 protein in MOLM-16 cells after 4 hr treatment and >50% of STAT3 protein in DEL, KI-JK and SU-DHL-1 cells after 7 hr treatment, also efficiently degraded STAT3 protein in murine cells.SD-36 displays extremely high cellular selectivity for degradation of STAT3 over other STATs.SD-36 effectively degrades both wild-type and mutated STAT3 proteins in cells, effectively degrades mutated STAT3 (D661Y, K658R mutant), also effectively degrades CRISPR-mutated homozygous Y705F mutant STAT3 protein in DLD-1/STAT3Y705F/Y705F cells.SD-36 displayed strong growth-inhibitory activities in a subset of leukemia and lymphoma cell lines (MOLM-16 cell line IC50, 35 nM), 100-fold more potent than SI-109.SD-36 (i.v. 25 mg/kg) effectively and selectively depletes STAT3 protein, achieves complete and long-lasting tumor regression in in mouse xenograft tumors.

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.

Highly selective inhibitor of the ​FK506-binding protein 51 (FKBP51)

BMS-195614 is a potent, orally bioavailable RARα antagonist (Ki = 2.5 nM) that modulates multiple signaling pathways. It upregulates Bcl2 expression while suppressing NF-κB, AP-1, and PPAR transactivation. Additionally, it reduces IL-6 and VEGF production, mitigates phototoxic damage from blue light, and exhibits anti-migratory, anti-inflammatory, and anti-angiogenic properties.

AZ3976 is a selective PAI-1 inhibitor that exhibits potent profibrinolytic effects, with IC50 values of 26 μM (chromogenic assay) and 16 μM (plasma clot lysis assay). Unlike conventional inhibitors, it does not target active PAI-1 but instead binds reversibly to the latent form, accelerating the transition of active PAI-1 to its inactive state.

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.

Novel Inhibitor of Monoubiquitinated Proliferating Cell Nuclear Antigen (PCNA), inhibiting Repair of Interstrand DNA Crosslink, enhancing DNA Double-strand Break, and sensitizing Cancer Cells to Cisplatin.

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.