Huib32 is a potent small-molecule inhibitor of USP32 (IC50 = 21.2 nM), exhibiting high selectivity over other closely related deubiquitinating enzymes (DUBs), such as USP8/10/16, UCHL1 and OTUB2. Huib32 reversibly inhibits USP32 by covalently binding to the active site Cys743, which enhances substrate ubiquitination, alters endosomal morphology, and mimics USP32 depletion. Huib32 can be used for breast, ovarian, and lung cancer and Alzheimer's and Parkinson’s diseases research.

JNJ-6640 is an inhibitor targeting mycobacterial PurF (the first enzyme in the de novo purine biosynthesis pathway) with potent anti-tuberculosis activity. JNJ-6640 exhibits bactericidal activity against Mycobacterium tuberculosis in vitro, with an MIC90 of 8.6 nM. JNJ-6640 disrupts de novo purine biosynthesis, inhibits M. tuberculosis DNA replication in vivo. JNJ-6640 exhibits anti-tuberculosis efficacy in acutely infected mice. JNJ-6640 can be used for the study of tuberculosis.

BMS-561388 (benzenesulfonate) is a corticotropin-releasing factor receptor (CRFR) antagonist. BMS-561388 (benzenesulfonate) can be used for the research of neurological disease, such as anxiety and depression.

MG-Lin1 is a molecular glucose degrading agent that targets the Lin28 protein. MG-Lin1 can significantly reduce the mRNA levels of let-7 targeting oncogenes. MG-Lin1 can significantly inhibit the migration ability of cancer cells. MG-Lin1 has no obvious cytotoxicity. MG-Lin1 can be used for cancer research.

Lin28 degrader MG-Lin2 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin2 significantly inhibit the migration ability of cancer cells. Lin28 degrader MG-Lin2 has no significant cytotoxicity. Lin28 degrader MG-Lin2 can be used for cancer research.

JQ-1-Azidopropylamine is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker, which recruits E3 ligases. JQ-1-Azidopropylamine can be used for synthesis of PROTAC JY-21

VU6008055 is a potent, selective, cross the blood-brain barrier and orally actively M4 positive allosteric modulator with EC50 values of 73.4, 19.5 nM for hM4, rM4, respectively. VU6008055 shows antipsychotic-like activity.

Iptriazopyrid (NC-656) is an azole carboxamide herbicide targeting 4-hydroxyphenylpyruvate dioxygenase (HPPD) with a Ki value of 24.3 nM for Arabidopsis HPPD and 33.3 nM for rice HPPD. Iptriazopyrid blocks plastoquinone and carotenoid synthesis, leading to weed chlorosis and death. Iptriazopyrid is promising for research of controlling weeds such as Echinochloa crus-galli in paddy fields.

XL-3156 is a potent, selective, and cross-species cGAS inhibitor. XL-3156 can simultaneously occupy both allosteric and orthosteric sites, and inhibit the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of autoimmune diseases, inflammatory conditions and other diseases.

DMP 904 is a noncompetitive full corticotropin-releasing factor receptor (CRFR) antagonist. DMP 904 can inhibit CRF-stimulated adenylate cyclase activity and ACTH release. DMP 904 exhibits anti-depressant and anti-anxiety activity.

EVT-101 free base is a GluN2B antagonist. EVT-101 free base binds at the same GluN1/GluN2B dimer interface as Ifenprodil. EVT-101 free base inhibits calcium influx in chicken-derived cells, with an EC50 of 22 nM. EVT-101 can be used in the research of brain disorders.

NGD 98-2 hydrochloride is an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist

GSK-958108 is a highly selective 5-HT1A receptor antagonist. GSK-958108 is commonly used in the study of neurological conditions.

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research.

SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC).

MolPort-002-705-878 is a highly selective FMS-like tyrosine kinase 3 (FLT3) inhibitor with a binding affinity of −11.33 kcal/mol. MolPort-002-705-878 inhibits the proliferation of FLT3-mutated acute myeloid leukemia (AML) cells. MolPort-002-705-878 is promising for research of FLT3-mutated AML.

NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis.

MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.

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.

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.