GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.

RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.

KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM.

DBPR114 is a quinazoline-based multi-kinase inhibitor for the treatment of acute myeloid leukemia and other solid tumors.

N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.

NMDAR/TRPM4 inhibitor 8 (Compound 8) is a neuroprotective NMDAR-TRPM4 interaction interface inhibitor but spare the critical healthy NMDAR function.

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors..

RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

CA77.1(CA) is a novel chaperone-mediated autophagy (CMA) activator for the treament of Alzheimer’s disease (AD).

Naxillin is the first non-auxin-like molecule that promotes root branching, activates a subset of auxin-induced transcripts, including AUX/IAA, SAUR and PIN families; induces auxin response in the basal meristem; represents a valuable tool to further decipher the molecular networks involved in lateral root branching.

XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.

MK-8153 is a potent and selective ROMK (potassium channel, Kir1.1) blocker with IC50 of 2.5 nM in rat ROMK, rKir1.1/HEK293 cells. MK-8153 has a longer projected human half-life (~14 h) than MK-7145, which should provide a reduced peak-to-trough exposure ratio and potentially, a smoother, more extended diuretic response.

DFP00173 (DFP-00173) is a potent and selective aquaporin-3 (AQP3) inhibitor, inhibits glycerol permeability in erythrocytes with IC50 of 0.2 uM..

4-Allylcatechol (4-Allylpyrocatechol, Hydroxychavicol) is an intermediate to synthetic safrole.

CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM.

LP-184 is a highly potent novel alkylating, next-generation analog of irofulven. LP-184 is an DNA damage repair (DDR) inhibitor and and shows broad anti-tumor cytotoxicity across a panel of NSCLC derived cell lines.

AZD8154 is a highly potent, inhaled dual PI3Kγ/PI3Kδ inhibitor with pIC50 of 9.1 and 8.4, respectively.

WRX606 is a nonrapalog inhibitor. WRX606 formed a ternary complex with FK506-binding protein-12 (FKBP12) and FKBP−rapamycin-binding (FRB) domain of mTOR, resulting in the allosteric inhibition of mTORC1. WRX606 inhibited the phosphorylation of not only the ribosomal protein S6 kinase 1 (S6K1) but also eIF4E-binding protein-1 (4E-BP1). Hence, WRX606 efficiently suppressed tumor growth in mice without promotion of metastasis. These results suggest that WRX606 is a potent lead compound for developing anticancer drugs discovered by in silico and in cell methods.

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis.

ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities.

Teplinovivint is a Wnt pathway inhibitor.

(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively).