HLQ2H (Msi3 inhibitor 2H) is a first-in-class, specific inhibitor of fungal Hsp110 molecular chaperone Msi3, inhibits the holdase activity of Msi3 (IC50=5.02 uM) as well as the growth and viability of C. albicans.

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. .

SHIN-2 is a novel SHMT inhibitor, increasing survival in NOTCH1-driven mouse primary T-ALL 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.

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg

MBX3132 is a small mocule inhibitor of AcrB multidrug efflux pump, fully potentiates the activity of a broad range of antibiotics at 0.1 uM; does not exhibit membrane-disrupting or antibacterial activity.

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

VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.

NuP-3 is a potent, selective MAPK13 and MAPK14 inhibitor with IC50 of 7 and 14 nM, respectively.

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

Dox-btn2 is a biotinylated derivative of Doxorubicin, with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.

ProSeAM is a chemical tool for methylome analysis.

Leucettinib-21 is a highly selective and potent dual inhibitor targeting both DYRK and CLK kinase families. It demonstrates nanomolar-level inhibitory activity, with IC50 values of 2.4 nM (DYRK1A), 6.7 nM (DYRK1B), 12 nM (CLK1), 33 nM (CLK2), and 5 nM (CLK4), respectively. This compound exhibits remarkable kinase selectivity, making it a valuable pharmacological tool for studying these kinase-mediated pathways.

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

THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.

Amastatin HCl is an aminopeptidase inhibitor that also induces vasoconstriction.

BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.

Phenylacetylglutamine is used as biomarker for metabolic age.

DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination treatments in cancer through inhibiting autophagy.

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.

KT-474 is a highly active and selective, orally bioavailable IRAK4 degrader being developed for the treatment of toll-like receptor (TLR)/interleukin-1 receptor (IL-1R)-driven immune-inflammatory diseases.