Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.

Tubulin inhibitor 1 is a tubulin inhibitor, occupying the colchicine binding site, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.

Trk-IN-4 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

TM-25659 is a TAZ modulator. Anti-osteoporotic and anti-obesity activities.

The less active enantiomer of GNE-140, inhibits LDHA activity (18-fold less potent that (R)-GNE-140).

TB500-2 is one of the TB500 metabolites. TB500 is a synthetic version of an active region of thymosin β4. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decreas

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent ROR isoforms selectivity (>5000-fold selectivity aga

TAK-700 shows potent inhibitory activity against rat, monkey, and human steroid 17,20-lyase inhibitor with IC50 of 54 nM, 27 nM, and 38 nM, respectively.

SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.

Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activ

BL-AD008 (BL-AD 008) is a novel small molecule, dual-target activator targeting AMPK/ZIPK; demonstrates remarkable anti-proliferative activities toward cervical cancer cells and could induce apoptosis by death-receptor and mitochondrial pathways; also sho

BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase with Ki of 7.5 nM, displays no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

A potent and selective VEGFR2 (KDR) inhibitor with IC50 of 40 nM.

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MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, wit

RO 27-3225 (RO27-3225, RO 273225) is a potent, selective melanocortin melanocortin receptor MC4R agonist with EC50 of 1 nM, >30-fold selectivity over MC3R.

SHP504 is a distinct, allosteric site 2 SHP2 inhibitor with IC50 of 21 uM (SHP2 1-525), and selective over the phosphatase domain (SHP2 PTP IC50>100 uM).downregulates DUSP6 mRNA, a downstream MAPK pathway marker, in KYSE-520 cancer cells.

JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.

BCH (LAT1-IN-1) is a selective and competitive inhibitor of system L amino acid transporter 1 (LAT1). BCH (LAT1-IN-1) induces apoptosis in cancer cells.

GSK805, also known as ROR gamma-t-IN-1, is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.

A-800141 is a potent, highly specific, orally bioavailable MetAP2 inhibitor with IC50 of 12 nM, shows no inhibition for MetAP1 (IC50>30 uM).

Tenofovir exalidex is a novel lipid acyclic nucleoside phosphonate that delivers high intracellular concentrations of the active antiviral agent tenofovir.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 18 nM and 69 nM for mouse sEH and human sEH, respectively.

Oseltamivir acid (GS 4071, Ro 64-0802, Oseltamivir carboxylate) is a potent inhibitor of influenza neuraminidase (NA) with Ki of <1 nM for both A and B strains,showed potent activity against COVID-19(SARS-COV-2).

Deoxynyboquinone, also known as DNQ, is a potent inducer of cancer cell death. DNQ potently induces death of cancer cells in culture, with IC(50) values between 16 and 210 nM. In addition, unlike the experimental therapeutic elesclomol, DNQ is still able to induce cancer cell death under hypoxic conditions. This mechanistic understanding of DNQ will allow for a more comprehensive evaluation of the potential of direct ROS generation as an anticancer strategy, and DNQ itself has potential as a novel anticancer agent.