oncogenic

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

UNC569 (UNC 569) is a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body. It is also a selective uric acid re-absorption inhibitor. UNC569 could normalize the amount of uric acid excreted by gout patients previously classified as under-excretors.

RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.

Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.

Lactate oxidase is an FMN-dependent enzyme that specifically catalyzes l-lactate, destroys lactate-activated RAS and PI3K oncogenic signaling, and can be used in the diagnosis and treatment of cancer.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

MS 39 is a potent Proteolysis Targeting Chimera (PROTAC) designed to degrade the Epidermal Growth Factor Receptor (EGFR). The molecule is composed of three structural motifs: an EGFR target ligand (red part), a VHL E3 ligase ligand (S,R,S)-AHPC (blue part), and an undecanedioic acid linker (black part). By facilitating the formation of a ternary complex between EGFR and the VHL E3 ubiquitin ligase, MS 39 triggers the polyubiquitination and subsequent proteasomal degradation of the receptor. MS 39 effectively reduces EGFR protein levels and inhibits downstream oncogenic signaling in HCC-827 and H3255 cell lines, leading to significant suppression of H3255 cancer cell proliferation.

G12Si-5 is a covalent inhibitor of the K-RasG12S mutant with a Ki value of 26 μM. It binds to the S-IIP structural domain, inhibiting oncogenic signaling and reducing ERK phosphorylation levels in KRAS G12S mutant cells.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

XMU-MP-2 is a potent and selective protease inhibitor with anticancer activity that inhibits the growth of oncogenic BRK-driven tumors in a mouse xenograft model.

PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf with IC50 of 13 nM.

Fumaric acid (2-Butenedioic acid) attenuates the eotaxin-1 expression in TNF-α-stimulated fibroblasts by suppressing p38 MAPK-dependent NF-κB signaling. Fumaric acid has recently been identified as an oncometabolite or an endogenous, cancer-causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Its oncogenic action appears due to its ability to inhibit prolyl hydroxylase-containing enzymes.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

ML399 is the menin--MLL interaction inhibitor that demonstrates strong and selective effects in MLL leukemia cells, and ML399 validates a specific mechanism of action by blocking oncogenic menin-MLL signaling, providing a valuable chemical probe for functional genomics and leukemia-targeted therapeutic strategy development while enabling comprehensive mechanistic and translational hematologic cancer research.

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

trans-Pralsetinib (trans-BLU-667) is a potent inhibitor of the RET (Rearranged during Transfection) kinase. This compound originates from Compound Example 129 in patent US20170121312A1. RET is a receptor tyrosine kinase whose genetic rearrangements or mutations are key drivers in various cancers, including non-small cell lung cancer (NSCLC) and medullary thyroid cancer. By inhibiting RET kinase activity, trans-Pralsetinib blocks downstream oncogenic signaling pathways, thereby exerting anti-tumor effects.

CMLD010509 (SDS-1-021) is a highly selective inhibitor of the oncogenic translation program that supports multiple myeloma (MM), targeting key oncoproteins such as MDM2, CCND1, MYC, MAF, and MCL-1.

PIM1-IN-1 is a potent and highly selective PIM kinase inhibitor with strong preference for PIM1 and PIM3 over PIM2, effectively inhibiting BAD phosphorylation without detectable effects on FLT3 or hERG binding, and exhibiting antiproliferative and anticancer activity suitable for mechanistic studies of PIM-driven oncogenic signaling.

Balamapimod, also known as MKI-822, is a small-molecule Ras/Raf/MEK inhibitor that directly targets deregulated MAPK signaling cascades and is being actively explored to suppress aberrant protein kinase activity implicated in oncogenic transformation, inflammatory signaling, and pathological cell proliferation, with demonstrated therapeutic relevance for stroke, osteoporosis, rheumatoid arthritis, polycystic kidney disease, colonic polyps, and other inflammation-driven disorders through pathway-level inhibition.

TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG, an oncogenic factor in acute myeloid leukemia. It impairs SCF ER-Hoxb8 cell differentiation in response to estrogen withdrawal.

BIX02188 is a selective and potent MEK5 inhibitor that inhibits MEK5-induced apoptosis in cells expressing the oncogenic mutant FLT3-ITD.

E3 ligase Ligand 18 is a small molecule ligand that specifically binds to E3 ubiquitin ligase, and E3 ligase Ligand 18 can be chemically linked to a protein-targeting ligand through a molecular linker to construct proteolysis-targeting chimeras (PROTACs), which subsequently induce ubiquitination-mediated degradation of disease-related proteins such as oncogenic factors, thereby supporting the study of targeted protein degradation in cancer biology.

6H05 (K-Ras inhibitor) is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C).