H-Tyr(SO2F)-OMe-18F, a 18F-fluorosulfurylated phenol, is a positron emission tomography (PET) tracer.

N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM.

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization[1][2].

F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.

Ezeprogind (AZP-2006) disulfate is an orally active neurotrophic inducer. Ezeprogind disulfate targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind disulfate is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.

Milvexian (BMS-986177), an effective antithrombotic agent, is an orally-bioavailable, reversible and direct inhibitor of human and rabbit factor XIa (FXIa) with Ki of 0.11, and 0.38 nM, respectively.

Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.

YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.

GDC0214 is a potent, selective inhalable and lung-restricted inhibitor of JAK1 with IC50 of 8.52 nM, displays 6.3/704/28 fold selectivity over JAK2/JAK3/TYK2.

Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis[1]. Isoxicam is a nonselective inhibitor of COX-1 and COX-2[2].

Azido-PEG23 amine is a PEG derivative containing an amino group with an azide group. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. PEG Linkers may be useful in the development of antibody drug conjugates.

Cariprazine (RGH-188) is a novel putative antipsychotic drug that exerts partial agonism at dopamine D2/D3 receptors, with preferential binding to D3 receptors, and partial agonism at serotonin 5-HT1A receptors.

CM 10 is an ALDH1A inhibitor that depletes CD133+ cancer stem cells.

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

β-catenin inhibitor C2 is a novel potent selective β-catenin inhibitor with Kd of 54.96 nM, directly to ARM domain of β-catenin.β-catenin inhibitor C2 reduced viability of DLD1 and SW480 cells in dose-dependent manner with IC50 ranging between 0.8-1.3 uM, viability of HCT116 and SW48 with IC50 3.45-5.35 uM.β-catenin inhibitor C2 selectively inhibits β-catenin, lowers its cellular load and significantly reduces viability of β-catenin-driven cancer cells.

ZY12201 is a potent, selective, orally bioavailable TGR5 agonist with hTGR5 EC50 of 57 pM and mTGR EC50 of 62 pM.ZY12201 displays a favorable pharmacokinetic properties and demonstrated in-vivo glucose lowering effects in animal models (ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg).

ZJU-37 is a novel small molecule, BBB penetrant RIPK1 kinase inhibitor (IC50=366.4 nM) with higher potency than Nec-1s, prevents TNFα-induced necroptosis of Jurkat FADD−/− cells with IC50 of 185.2 nM.ZJU-37 promotes oligodendrocyte progenitor cells (OPCs) proliferation in vitro with higher efficacy than Nec-1s, enhances remyelination in vivo.ZJU-37 promotes transcription of PDGFRα and proliferation of OPCs via NF-κB.

ZH07 (Dual Mcl-1/Bfl-1 inhibitor 24) is a potent, selective dual Mcl-1 and Bfl-1 inhibitor, binds both Mcl-1 and Bfl-1 with Ki of 97 nM and 100 nM, respectively.ZH07 displays appreciable selectivity (>250-fold) over Bcl-2/Bcl-xL.ZH07 induces dose-dependent disruption of interactions between BL-Bim and endogenous Mcl-1 and Bfl-1, without affecting the complexes between BL-Bim and Bcl-2 or Bcl-xL.ZH07 demonstrates on-target cellular activity in model lymphoma cell lines.

Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual CB1 receptor/iNOS inhibitor.Zevaquenabant ((S)-MRI-1867) (3 mg/kg, p.o.) ameliorated obesity-induced kidney morphological and functional changes via decreasing kidney inflammation, fibrosis, oxidative stress, and renal injury.The hybrid CB1R/iNOS inhibitor Zevaquenabant ((S)-MRI-1867) has greater antifibrotic efficacy than inhibition of CB1R alone.(S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diet-induced obesity (DIO mice).

Zebularine (NSC309132, 4-Deoxyuridine) is a nucleoside analog of cytidine and inhibitor of cytidine deaminase, also inhibits DNA methylation and tumor growth both in vitro and in vivo.

ZE132 is a potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of <0.1 nM.ZE132 effectively inhibits the PD-1/PD-L1 interactions in vitro, and has a potent affinity to PD-L1.ZE132 shows robust anti-tumour effects in vivo, better than anti-PD-1 antibody.ZE132 treatment promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression.ZE132 elicits strong inhibitory effects on the mRNA expression of TGF-β.

ZB-R-55 is a potent and selective RIPK1 inhibitor with IC50 of 5.7 nM, 10-fold more potent than GSK2982772.ZB-R-55 is a dual-mode RIPK1 inhibitors occupying both the allosteric and the ATP binding pockets.ZB-R-55 exhibits excellent kinase selectivity, good oral pharmacokinetics and good therapeutic effects in the LPS-induced sepsis model.

YX-I-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically inhibits amyloid formation; YX-I-1 inhibits the aggregation of wt hIAPP, extending the t50 from 15.1 ± 0.2 h to 23.4 ± 1.0 h at a 1:7 molar ratio of peptide:inhibitor. YX-I-1 inhibits primary nucleation, secondary nucleation and elongation of wt hIAP. YX-A-1 is a useful chemical tools to study hIAPP aggregation.

YX-A-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically enhances amyloid formation; YX-A-1 accelerates wt hIAPP assembly, even when added in substoichiometric concentration ratios (e.g. at a peptide:YX-A-1 molar ratio of 1:0.5 the t50 is reduced ~1.5-fold). YX-A-1 is a useful chemical tools to study hIAPP aggregation.

YX-2-115 is a palbociclib derivative compound with piperazine-linker tail for PROTAC YX-2-107 synthesis, inhibits CDK6 with IC50 of 4.5 nM.

YTX-7739 is a potent, selective stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 12 nM.YTX-7739 concentration-dependently reduces the fatty acid desaturation index (FADI), the ratio of monounsaturated to saturated fatty acids, with potential to treat synucleinopathies.

YTK-105 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YTK-105 for AUTOTAC design.

YTK-105 is a small molecule p62-ZZ domain ligand, activate p62-dependent selective macroautophag, used for AUTOTAC design.

YQ-0629 is a specific HIF-2α inhibitor, binds to HIF-2α PAS-B domain with Kd of 57.5 uM.YQ-0629 could inhibit the expression of HIF-2α with or without the presence of PTX (3 nM) in MCF7 MS culture, does not bind to HIF-1α or affect the expression of HIF-1α.YQ-0629 suppresses self-renewal capacity and synergizes with PTX to reverse the chemoresistance of MCF7 MS.YQ-0629 inhibits growth of BCSCs derived from breast cancer patients and synergistically increases anti-BCSCs activity of PTX in vivo.

YOK-2204 linker conjugate 1 is a PEG linker added to p62-ZZ ligand YOK-2204 for AUTOTAC design.