RPL11-MDM2 inhibitor S9 (J012-3168) is a small-molecule RPL11 mimetic and potential inhibitor of RPL11-MDM2 interaction, directly binds MDM2 and induces p53 stabilization and activation.

A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist.

Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.

GYS32661 is a potent, small-molecule inhibitor of RAC1 and its isoform RAC1B, specifically designed to target the Sonic Hedgehog (Shh) signaling pathway in cancers like medulloblastoma and colorectal carcinoma. Distinguishing itself from other RAC1 inhibitors, GYS32661 exhibits exceptional blood-brain barrier (BBB) permeability with an approximately 50% brain-to-plasma ratio, making it a premier candidate for treating CNS-related malignancies. It functions by disrupting the activation of RAC1 (IC50 ≈ 1.18 μM), subsequently reducing the expression of downstream transcription factors GLI1 and GLI2, which effectively halts tumor proliferation and metastasis. In preclinical in vivo models, the compound has demonstrated significant anti-tumor efficacy and a favorable safety profile without systemic toxicity. Due to its hydrophobic nature, it is typically formulated in a vehicle of DMSO, PEG300, and saline for administration. As a non-toxic clinical candidate, GYS32661 represents a promising therapeutic strategy for overcoming chemoresistance and improving survival rates in Shh-driven pediatric and adult tumors.

LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy.

DF-003 is a selective, orally active, ATP-competitive, and brain-penetrant ALPK1 inhibitor. DF-003 potently inhibits human ALPK1 and ALPK1[T237M] with IC50s value of 1.5 nM and 16 nM. DF-003 exhibits more than 860-fold selectivity over the closest kinase. DF-003 inhibits TNF, CXCL10, or CXCL8 upregulation in HEK-293 cells. DF-003 can be used for the study of retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache (ROSAH) syndrome.

DF-006 is a small molecule, orally active Alpha-kinase 1 (ALPK1) agonist, activates ALPK1 and stimulates host innate immunity locally in liver, DF-006 enacts potent anti-HBV responses in mouse models of HBV and in primary human hepatocytes.

PD-1/PD-L1 inhibitor 1 is a PD-1/PD-L1 interaction inhibitor,IC50 values: 0.006-0.10 μM,a useful immunomodulator compound.

RSL3-NH2 is a GPX4 inhibitor and Ferroptosis inducer. RSL3-NH2 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).

Amenamevir, also known as ASP2151, is a herpes virus helicase-primase inhibitor.

A pan-RAR inverse agonist that blocks RARα activity with IC50 of 114 nM.

DAPT(GSI-IX) is an inhibitor of γ-secretase; DAPT causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma.

AH001 is a orally active RhoA inhibitor, which binds a cryptic pocket proximate to GDP within RhoA with a KD of 73.16 nM. AH001 interacts with GDP, stabilizing RhoA’s interaction with its endogenous inhibitor, RhoGDIα. AH001 reduces the downstream MRTFA nuclear translocation and downregulates fibrosis/hypertrophy proteins. AH001 mitigates myocardial remodeling in multiple HF animal models, and in the 3D myocardial tissue model. AH001 exerts its cardioprotective effects through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signaling.

CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity.

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increase tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC).

Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth.

NuP-3 is a potent and selective MAPK13 and MAPK14 inhibitor (IC50 of 7 nM and 14 nM, respectively) that effectively targets respiratory inflammation and mucus overproduction. In human tracheal epithelial cell (hTEC) cultures, it markedly inhibits IL-13-induced MUC5AC and CLCA1 expression without causing cell toxicity, showing superior efficacy compared to the MAPK14 inhibitor NuP-43. Beyond its success in minipig models of airway disease and viral infection, NuP-3 also down-regulates biomarkers associated with basal-epithelial stem cell activation, demonstrating its role as a precise upstream therapeutic agent for chronic lung conditions.

BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL).

BPH-1358 mesylate (NSC50460 mesylate) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively. BPH-1358 mesylate is active against S. aureus in vitro (MIC ~250 ng/mL).

Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4

T0080 is a FPR-1 antagonist. T0080 reduces the cell apoptosis, inhibits ROS production and pro-inflammatory cytokines (TNF-α and IL-1β) from plaque macrophages, which attenuates atherosclerotic progression in ApoE−/− mice.

MitoCKi (Creatine kinase inhibitor CKi-26) is a selective, covalent inhibitor of creatine kinases (CKs), inhibits recombinant creatine kinase B (CKB) phosphotransfer activity with IC50 of 185 nM, depletes creatine phosphagen energetics in cells.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM.

GSK-3923868 (PI4KB inhibitor 30) is a potent, selective, slow-dissociating PI4KB (PI4kIII-beta) inhibitor with pKi of 9.8, >1000-fold selectivity over PI4KA, inhibits HRV viral replication in COPD BECs.

T26A is a competitive prostaglandin transporter (PGT) inhibitor (Ki=378 nM). T26A is promising for research of prostaglandin signaling and inflammatory diseases (e.g., glaucoma, pulmonary hypertension) .

HQY426 is a specific, orally bioavailable inhibitor of pre-messenger RNA endonuclease cleavage and polyadenylation specificity factor 3 (CPSF3) with binding IC50 of 0.32 uM, exhibits potent antitumor activity.

LDN-0130436 is a novel TDP-43::GFP aggregation inhibitor.

IBS007125 is a small molecule inhibitor of c-Maf, inhibits multiple myeloma proliferation by targeting cMaf transcriptional activity.

KDOBA67 is a novel cell-permeable inhibitor of H3K27 lysine demethylase KDM6A/B, inhibits TBXT expression chordoma cell lines.KDOBA67 displayed in vitro inhibitory activity in the low micromolar range with IC50 values of 2 to 5 uM in various chordoma cell lines, leading to induction of apoptosis.H3K27 demethylase inhibition via KDOBA67 alters chromatin state at TBXT and inhibits its expression.TBXT was a KDM6A/B target gene, and chromatin changes at TBXT following KDOBA67 treatment were associated with a reduction in TBXT protein levels.KDOBA67 treatment downregulated expression of a network of transcription factors critical for chordoma survival and upregulated pathways dominated by ATF4-driven stress and proapoptotic responses.