MT-125 is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.

VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research.

BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.

MePT-S-N-Pme is an inhibitor of SARS-CoV-2 RdRp activity. MePT-S-N-Pme demonstrates a significant reduced reporter activity with an IC50 of 7 μM in HEK 293 cells. MePT-S-N-Pme has a slight inhibitory effect on nucleotidyltransferase activity. MePT-S-N-Pme significantly inhibits SARS-CoV-2 replication in vitro.

SK60 is a dimethylated derivative of GSK321 with low nanomolar potency and high selectivity for IDH1R132H (IC50 = 14.5 nM). SK60 can be used as a tracer for brain imaging with the fluorescent label [18F].

INCB126503 is an orally activeM, selective FGFR2/3 Inhibitor with IC50 values of 70 nM (FGFR1), 2.1 nM (FGFR2), 1.2 nM (FGFR3), 0.92 nM (FGFR3-V555L), 0.85 nM (FGFR3-V555M) and 64 nM (FGFR4). INCB126503 suppresses FGFR signaling in vivo without causing hyperphosphatemia and shows antitumor efficacy in xenograft models harboring FGFR3 genetic alterations.

MR24 TFA, a G-5555 derivative, is a mammalian STE20-like (MST) kinase inhibitor. MR24 TFA shows selectively to MST3/4 over MST1/2, with EC50 values of 57 and 583 nM, respectively. MR24 TFA induces G1 phase cell cycle arrest. MR24 TFA can be used for cancer research, such as breast, liver and lung cancers.

AN-132 (phosphate) is an antiarrhythmic agent. AN-132 (phosphate) can inhibit Sodium Channel. AN-132 (phosphate) can prolong atrioventricular conduction time, decrease sinus rate and reduce the force of papillary muscle contraction. AN-132 (phosphate) can be used for the research of cardiovascular disease.

PSB-22219 is a highly selective non-nucleotidic ligand acting on P2Y12 receptors (KD=4.57 nM). PSB-22219 is promising for research of P2Y12 receptor-associated neuroinflammation.

MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pockeet of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model.

FLM-5011 is a lipoxygenase inhibitor. FLM-5011 can diminish myocardial ischaemia injury and shows anti-inflammatory effect. FLM-5011 can be used for the researches of inflammation and cardiovascular disease, such as myocarditis.

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.

Gamhepathiopine is a thienopyrimidinone compound. Gamhepathiopine exerts antimalarial effects by targeting the Qo site of Plasmodium falciparum cytochrome b and inhibiting the activity of complex III in the electron transport chain.

dRRM-1 is a DCAF15-dependent molecular glue degrader of RBM39 and RBM23. dRRM-1 can rescue the self-degradation of DCAF15. dRRM-1 can be used for the research of cancer.

BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research.

BIRB-1017 is a potent inhibitor of p38 MAP kinase. BIRB-1017 can be used in inflammation research.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.

4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine.

ECC-5004 (Compound 1) is a GLP-1 receptor agonist with an EC50 of 0-20 nM. ECC-5004 exhibits strong inhibitory effects on OATP1B1, with an IC50 < 1 μM. ECC-5004 can be used to study diseases such as diabetes, obesity, and non-alcoholic fatty liver disease.

Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B.

TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.

dAPM-1 (acetate) is a peptidomimetic antibiotic agent. dAPM-1 (acetate) can selectively induces intracellular aggregation in B. subtilis. dAPM-1 (acetate) is active against S. aureus, methicillin-resistant S. aureus (MRSA), B. subtilis, E. faecium, and M. smegmatis with MICs of 8, 4, 4, 8, and 16 µg/ml, respectively.

(3S,4R)-ME-344 is the (3S,4R)-enantiomer of ME-344). ME-344 is a mitochondrial Heme oxygenase 1 (HO-1) inhibitor. ME-344 specifically binds and alters HO-1 structure, and increases HO-1 translocation from the rough endoplasmic reticulum to mitochondria, but only in drug-sensitive cells (such as H460 and SHP-77 cells). ME-344 decreases mitochondrial ATP production and induces ROS, with subsequent disruption of redox homeostasis and mitochondrial function. ME-344 has significant antitumor activity, and can be used for cancers like breast cancer research.

YTHDF2 ligand-1 (Compound 23) is a selective and high-affinity YTHDF2 ligand with a Kd of 1.3 μM (FP assay) and an IC50 of 11 μM (HTRF assay) . YTHDF2 ligand-1 can be used in the study of cancer.

MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors.

Debio 1453 is a bactericidal FabI inhibitor potent against N. gonorrhoeae (IC50 = 0.6 nM), including drug-resistant strains. Debio 1453 demonstrates a low propensity for resistance selection and is effective in eradicating both planktonic and intracellular bacteria through a mechanism of concurrently inhibiting FabI and engaging the non-mutable NADH cofactor. Debio 1453 clears antibiotic-resistant N. gonorrhoeae infection in a murine vaginal model. Debio 1453 can be used for gonorrhoea research.

14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research.

AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers.

HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases.

1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc is a phospholipid-porphyrin conjugate. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc can be utilized in photodynamic therapy research.