AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).

ZSA-51 is a potent and orally active STING agonist. ZSA-51 shows anticancer activity. ZSA-51 remodeles immune microenvironment both in tumor and lymph node.

SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM.

T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.

A novel mitochondrial and mTOR inhibitor with potent anti-cancer activity, inhibits leukemia cell lines with IC50 of 70-260 nM.

PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.

PITCOIN2 (LU-06-006) is a potent selective PI3KC2α inhibitor with IC50 of 126 nM, has selectivity against PI3KC2γ but shows micromolar activity on PI3KC2β.

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.

(3S) ALG-05 is a potent pan-inhibitor of gut microbia tryptophan-indole-lyases (TILs, E.C. 4.1.99.1), exhibits inhibitory activity across TILs with Ki of 7-11 uM.

Biliverdin hydrochloride is a tetrapyrrolic, water-soluble compound formed by the breakdown of heme. Biliverdin hydrochloride can upregulate the activity of biliverdin reductase which is an enzyme that is a regulator of the innate immune system.

PXS-5505 is a lysyl oxidase inhbitor. DWN63831 may be useful in treatment of a variety of disorders, e.g., fibrosis, cancer and angiogenesis in human subjects as well as in pets and livestock. DWN63831 was first reported in patent WO 2020024017.

Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

OV329 (OV 329) is a highly potent inactivator of gamma-aminobutyric acid aminotransferase (GABA-AT) with Ki of 9.69 uM.

TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.

Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss

ARC39 is acid sphingomyelinase inhibitor (IC50 =20 nM).

Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.

A potent, selective inhibitor of HIV integrase (IC50=8-15 nM) with potent antiviral activity in cell culture and good pharmacokinetic properties.

MYC-IN-2 is a MYC protein-protein inhibitor. MYC-IN-2 can be used for the research of cancer.

Secreted frizzled-related protein-1 (sFRP-1) modulaitor

NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.

3-Methoxy PCE (3-MEO PCE) hydrochloride is structurally classified as an arylcyclohexylamine and is an /b>NMDA receptor antagonist with a pKi value of 7.22.

AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers.

PAANIB-1 is a brain-penetrant PAAN/MIF nuclease inhibitor that prevents neurodegeneration that prevents neurodegeneration induced by α-syn PFF, AAV-α-syn overexpression, or MPTP intoxication in vivo.

Pomalidomide-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.

Thalidomide-amido-PEG2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

(S,R,S)-AHPC-C1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.

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.

Thalidomide-NH-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

GDC-2992 (Compound 28A) is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.