ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC50 value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc.

G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.

Repibresib (VYN201) is a bromodomain and extra-terminal motif (BET) inhibitor. Repibresib shows antineoplastic activity.

INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases.

BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions.

CAT335 is a TREK activator. CAT335 can be used in the research of pain sensation, sleep, and intraocular pressure.

TC9-305 is a potent and selective apoptosis inhibitor. TC9-305 has strong inhibitory activity against both Bim and tBid-induced apoptosis with EC50 values of 0.42 and 0.23 μM. TC9-305 can maintain the mitochondrial membrane potential, reduce ROS production, prevent the release of cytochrome c and block the upstream pathways of mitochondrial-mediated apoptosis. TC9-305 can be used for the research of neurological disease, such as storke.

c-Met ligand-Linker Conjugate 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for c-Met and a PROTAC linker, which recruits E3 ligases. c-Met ligand-Linker Conjugate 1 can be used for synthesis of PROTAC c-Met degrader-5

LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC50 = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis.

KLYP961 is a selective and orally active dual inhibitor of inducible and neuronal NO synthase (IC50 = 50-400 nM). KLYP961 can inhibit endotoxin-evoked plasma nitrates increases and attenuate pain behaviors in a mouse formalin model. KLYP961 can attenuate carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by Phenylbenzoquinone. KLYP961 can be used for the research of neurological disease.

MEN-91507 is an orally activecysteinyl leukotriene receptor 1 (CysLTR1) receptor antagonist. MEN-91507 behaves as insurmountable antagonist of Leukotriene D4)-induced calcium transients, with a pKb of 10.25. MEN-91507 can inhibit Leukotriene D4-induced bronchoconstriction and microvascular leakage in guinea-pigs. MEN-91507 can be used for the researches of inflammation, immunology.

Y040-7904 is a mitophagy activator. Y040-7904 enhances mitophagy by promoting mitochondria transport to autophagosomes and the fusion of autophagosomes with autolysosomes. Y040-7904 induces mitophagy through the SIRT1/FoxO3 pathway. Y040-7904 upregulates the levels of Parkin, PINK1, and LC3II/I. Y040-7904 reduces amyloid-β (Aβ) accumulation in both in vitro and in vivo models of Alzheimer’s disease.

K-832 is an orally active IL-1β secretion inhibitor. K-832 can be used in the research of rheumatoid arthritis.

VU0514009 is a competitive chemokine-like receptor 1 (CMKLR1) antagonist (EC50=2 nM). VU0514009 prevents chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca2+ flux response in HEK293 cells. VU0514009 is promising for research of inflammatory diseases and metabolic syndrome.

KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.

GSM III is a γ-Secretase complexe (GSEC) modulator. GSM III significantly regulates amyloid-β (Aβ) length at the extracellular interface between the protease (NCT, PSEN) and the substrate APPC99. GSM III can be used for Alzheimer's disease (AD) research.

3'2'-cGAMP (c[A(2',5')pG(3',5')p]) disodium is the disodium of 3'2'-cGAMP). 3'2'-cGAMP (c[A(2',5')pG(3',5')p]) is a cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) isomer. 3'2'-cGAMP exhibits high selectivity for Drosophila STING (dSTING), activating the dSTING-NF-κB signaling pathway, inducing the expression of Sting-regulated genes (Srg) and conferring a potent antiviral state in vivo. 3'2'-cGAMP is resistant to cleavage by viral poxins. 3'2'-cGAMP can be used for the study of viral infections.

3'2'-cGAMP (c[A(2',5')pG(3',5')p]) is a cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) isomer. 3'2'-cGAMP exhibits high selectivity for Drosophila STING (dSTING), activating the dSTING-NF-κB signaling pathway, inducing the expression of Sting-regulated genes (Srg) and conferring a potent antiviral state in vivo. 3'2'-cGAMP is resistant to cleavage by viral poxins. 3'2'-cGAMP can be used for the study of viral infections.

Lepetegravir (Example 24) is a HIV integrase inhibitor. Lepetegravir has antiviral effects (EC50: 0.98 nM in MT-4 cells).

CRBN ligand-8-O-C6-NH2 is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand and a linker. CRBN ligand-8-O-C6-NH2 can be used for synthesis of PROTAC ERα Degrader-11.

DRF-4848 is a COX-2 inhibitor. DRF-4848 can be used for the research of inflammation.

CW8001 is a covalent XPO1 (Exportin-1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. CW8001 prevents nuclear localization of NFAT transcription factors, suppressing expression of inflammatory cytokines like IL-2. CW8001 is promising for research of T cell-driven immune diseases such as graft-versus-host disease (GVHD).

AKI-001 is an inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes.

RBN010860 (example 150) is a potent PARP7 inhibitor with an IC50 of <0.1 μM. RBN010860 can be used for the study of cancer.

CST651 (PROTAC CDK4/6 degrader 34) is a selective cyclin dependent kinase CDK4/6 PROTAC degrader. CST651 can degrade CDK4 and CDK6 in MM.1S cells with DC50 values of 20 and 5.1 nM. CST651 can inhibit cancer cells proliferation and migration. CST651 can be used for the research of cancer, such as acute lymphoblastic leukemia.

Dalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer.

Mansonone E (Compound 5) is a pesticide. Mansonone E can be isolated from heartwood of Mansonia gagei. Mansonone E has significant antifungal activity against Cladosporium cucumerinum, Candida albicans and Phytophthora parasitica. Mansonone E has potent antibacterial activity with MIC50s of both 7.8 μg/mL for Xanthomonas oryzae pv. oryzae and X. oryzae pv. Oryzicola. Mansonone E also has antifeedant and herbicidal activities.

FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels.

Forvisirvat (SP-624) is an orally active, brain-penetrant and selective sirtuin 6 (SIRT6) activator. Forvisirvat activates the deacetylase activity of SIRT6, enhancing DNA repair and mitochondrial health, and exhibits antidepressant activity in animal models. Forvisirvat is promising for research of major depressive disorder.

NK-611 is an epipodophyllotoxin derivative. NK-611 induces DNA double-strand breaks by inhibiting topoisomerase II (IC50 = 56 μM). NK-611 does not inhibit microtubule polymerization, thus avoiding the side effects of the parent compound, Podofilox. NK-611 exhibits broad-spectrum antitumor activity and demonstrates potent efficacy in in vivo models of leukemia. NK-611 can be used in cancer research.