DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.

Peptide P60 (FOXP3 inhibitor P60) is a 15-mer synthetic peptide, cell-permeable inhibitor of FOXP3, binds specifically to FOXP3; inhibits murine and human-derived Treg and improves effector T cell stimulation, overcomes the inhibitory effect of FOXP3 on the activity of the transcription factors NF-κB and NFAT, inhibits upregulation of mRNA for Foxp3 and IL-10 on effector T cells and enhances mRNA for IFN-γ after anti-CD3 stimulation; induces a scurfy-like disease in newborn mice, improves vaccine efficacy in mice model of CT26 tumor and HCV infection.

ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.

PSB-16671 is a novel orthosteric and allosteric activator of GPR84, activates human GPR84 with EC50 of 41.3 nM in cAMP accumulation assays. PSB-16671 is selective versus related fatty acid receptors and the arylhydrocarbon receptor. PSB-16671 shows an EC50 of 5.47 uM in β-Arrestin assays, and allosteric KB value of 634 nM.

GB111-NH2 (Z-Phe-Lys-AOMK) is a novel cysteine cathepsin inhibitor that blocks the activity of cathepsins B, L and S. GB111-NH2 (Z-Phe-Lys-AOMK) inhibits autophagy and increases oxidative stress, specifically trigger macrophage cell death.

A novel and seletive HDAC6 inhibitor.

SP 600125, negative control (SPM1) is an alkyl derivative of pyrazoloanthrone, which can be used as a negative control for SP600125.

GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins.

SU-909 (SU909, IKKα-IN-48) is a potent, selective IKKα inhibitor with Ki of 0.08±0.07 uM, 10-20-fold selectivity over IKKβ (IC50=1.0±0.28 uM); inhibits FCS-stimulated phosphorylation of p100 in U2OS cells with IC50 of 8.8 uM, inhibits the noncanonical NF-kB pathway without affecting IKKβ-dependent IKappa-Bα loss in the canonical pathway.

First reported nonpeptidomimetic agonist on the G protein-coupled chemokine receptor CXCR-3

A peptidic glucagon like peptide 2 (GLP-2) analogue for treatment of type2 diabetes..

MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy. MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complex. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 reduces the PINK1 substrate pS65-Ubiquitin (pUb) in primary neurons and in vivo. MTK458 drives clearance of pathologic α-synuclein in vitro and in vivo, decreases pS129 α-synuclein aggregates and normalized both brain and corresponding plasma pUb levels in both cellular and animal models of α-synuclein aggregation (PD-like pathology).

TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide.

Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).

LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members.

CPI-0610 is a small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor CPI-0610 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth.

Protein E7(43-62) is an E7-derived peptide with anti-tumor effects (short peptide spanning the 43th to 62th amino acid residues in the E7 protein).

AMT hydrochloride is a selective inhibitor of inducible NOS (iNOS) with Ki of 4.2 nM.

AI-10-104 is a small molecule inhibitor that interferes with CBFβ binding to RUNX proteins with IC50 of 1.25 uM in FRET assays.

JP-11646 is a novel potent, selective, non-ATP competitive Pim2 inhibitor with IC50 of 0.5/1/24 nM for Pim2/3/1, respectively; shows less potency for other kinases in a kinase selectivity panel; exhibits 4-760-fold greater suppression of MM proliferation and viability than ATP-competitive PIM inhibitors; significant reduces tumor burden and increases median survival in xenogeneic myeloma murine models.

ARUK2001607 is a potent, selective and brain penetrant PI5P4Kγ inhibitor with binding KD of 7.1 nM, pIC50 of 7.1 (PI5P4Kγ+).

TD-1473 (Izencitinib, TD1473, JNJ 8398) is a potent, selective, oral gut-selective pan-JAK inhibitor with pKi of 10.0/10.0/8.8/9.5 for human recombinant JAK1, JAK2, JAK3 and TYK2.TD-1473 inhibited cytokine-induced phosphorylation of STAT1 in mouse primary colonic epithelial cells with pIC50 values for inhibition against IL-6, IFNα and IFNγ were 7.3, 6.8 and 7.0.TD-1473 demonstrated JAK inhibitory activity in ex vivo mouse colon and human IBD patient colonic tissue. TD-1473 (Izencitinib) is under development for the treatment of ulcerative colitis.

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

NCGC 00067819 is a small molecule compound that potentiates CREB signaling with EC50 of 16 nM in the primary screen and 79 nM in the CHO CRE-β-lactamase confirmation assay.

VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).VK-II-86 exhibited >2,000-fold lower beta-AR binding affinity than carvedilol.VK-II-86 prevented stress-induced ventricular tachyarrhythmias in RyR2-mutant mice and did so more effectively when combined with either of the selective beta blockers metoprolol or bisoprolol.VK-II-86 prevented hypokalaemia-induced AP prolongation and depolarization but did not alter AP parameters in normokalaemia.

Novel glucocerebrosidase activator; Non-inhibitory chaperones of glucocerebrosidase

Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.

PF-05381941 (PF 05381941, PF05381941) is a potent, dual TAK1/p38a inhibitor with IC50 of 156/186 nM respectively, with good kinome selectivity against 50 representative kinases.

FOBISIN 101 is a small molecule 14-3-3 protein-protein interaction inhibitor with IC50 of 9.3 and 16.4 uM for the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively.

2-Nitrosopyridine is a nitroso compound can be used to synthesize antibiotics.