L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia.

GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochlorid

NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 bind

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.

ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.

AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a drug used to treat cystic fibrosis that binds ΔF508-CFTR.

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.

XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent monomethyl auristatin E. Disitamab vedotin enhances antitumor immunity.

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).

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.

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