PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor. PF-06835919 is reported in patent US 20170183328 A1, example 4. Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose metabolism, identification of a selective KHK inhibitor may help to further elucidate the effect of KHK inhibition on these metabolic disorders.

Vonafexor (EYP001) is a selective FXR agonist with anti-HBV effects.

Pax2 inhibitor EG1 (EG1) is a potent, small molecule inhibitor of Pax2 mediated transcription activation, effectively blocks Pax2 activity and DNA binding with Kd of 1.35-1.5 uM; inhibits Pax2 mediated expression with IC50 of 10 uM, and inhibits proliferation of Pax2 positive renal and ovarian cancer cell lines but has little effect on Pax2 negative cancer cells; inhibits embryonic kidney development.

Dac590 is an orally active FTO inhibitor. Dac590 has a robust antiproliferative effect on AML cells, and induces apoptosis and cell cycle G1 arrest by inhibiting oncogenic FTO signaling. Dac590 significantly inhibits tumor growth and prolongs survival with no observed toxicity in acute myeloid leukemia (AML) xenograft mcie model, and shows a synergistic effect combined with Decitabine (HY-A0004).

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).

Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties.

GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.

GLPG4970 is a highly potent dual SIK2/SIK3 inhibitor with IC50 of 0.3 nM and 0.7 nM, with more than 100-fold selectivity against SIK1.

JWP24 is the first cell-permeable peptide inhibitor of MAGE-A4. JWP24 effectively disruptes the interaction between MAGE-A4 and RAD18, exhibiting an IC50 of 200 nM in a TR-FRET displacement assay and 0.5 μM in a NanoBRET cellular assay.

C210 is a novel HSP90 inhibitor, which overcomes doxorubicin (DOX) resistance of quiescent breast cancer cells by targeting TRAP1. C210 blocks the fragile energy flux of quiescent breast cancer cells prevalent in solid breast cancer tissue by dual inhibition of TRAP1 and HSP90α.

MG-101 is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines.

MG-115(MG 115) is an inhibitor of NFκB in the cytoplasm by acting on IKK or the proteasome.

Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor.

Vinorelbine is a semi-synthetic Vinca alkaloid which is currently used in treatment of different cancer types mainly advanced breast cancer (ABC) and advanced/metastatic non-small cell lung cancer (NSCLC). Vinorelbine-loaded SSM can be developed as a new,

An allosteric, sepecific inhibitor of substrate recognition by the SCFCdc4 ubiquitin ligase with IC50 of 6.2 uM in FP assyas.

NP161 is a potent and selective inhibitor of extracellular TRX (Thioredoxin 1) in vitro with IC50 of 0.54 uM.

ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human cell line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.

Zafirlukast(Accolate)

Potent inhibitor of protein arginine methyltransferases (PRMTs)

MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin.

STK018404 is a small molecule inhibitor of RNA-binding protein human antigen R (HuR), decreases the binding of HuR to its target RNA motif.

MC-VC-PAB-Azide is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

DBCO-S-S-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

MRT-3486 (Compound 5) is a cereblon-based NEK7 molecular glue degrader. MRT-3486 can be used for autoinflammatory diseases research.

D-TLKIVWI is a kind of d-enantiomeric peptide (D-peptide), which disassembles tau fibrils extracted from the autopsied brains of patients with AD (AD-tau), neutralizing the fibrils' seeding ability and rescuing behavioural deficits in a mouse model of AD.

m-PEG7-CH2COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

4A3-SCC-PH is a groundbreaking linker-degradable ionizable lipid (LDIL) that features a glutathione (GSH)-responsive cone-shaped molecular structure. This unique architecture enables superior endosomal escape and rapid mRNA release, making it highly effective for mRNA delivery. In vivo studies have highlighted its exceptional performance, showing a 176-fold increase in mRNA delivery efficiency to the liver compared to DLin-MC3-DMA, a widely used benchmark lipid. Both 4A3-SCC-PH and its structural analog, 4A3-SCC-10, also demonstrated significantly enhanced mRNA delivery efficacy compared to their non-disulfide-containing parent compounds and disulfide-containing controls with modified lipid tails.