oncogenic

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

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.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

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.

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

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

Onalespib (AT13387) is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.

SI-113 is a potent and selective inhibitor of SGK1, a serine threonine protein kinase, that modulates several oncogenic signaling cascades.

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of the oncogenic K-Ras(G12C) protein.

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.

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.

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

KT D606 is a PAK kinase family inhibitor with an IC50 of 4 μM. It selectively inhibits the proliferation of cancer cells transformed by oncogenic RAS mutants, making it useful for studying RAS PAK1-induced cancers.

WK88-1, an inhibitor of Hsp90, effectively induces the degradation of various oncogenic signaling molecules, including EGFR, ErbB2, and ErbB3, in the gefitinib-resistant H1975 cell line. This leads to subsequent growth arrest and apoptosis.

SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It selectively targets the mIDH2 R140Q protein with a potent inhibitory effect (IC50=4.78 nmol L), significantly reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum, and tumors. SH1573 is utilized in the study of acute myeloid leukemia (AML).

CCT070535 inhibits TCF-dependent transcription at the TCF level, displaying GI50 values of 17.6 μM in HT29 (APC mutation), 11.1 μM in HCT116 (oncogenic β-catenin), 11.8 μM in SW480 (APC mutation), and 13.4 μM in SNU475 (Axin mutation) cells.

XMD15-44, a RET kinase inhibitor, demonstrates potent growth-inhibitory effects on RAT1 cells transformed by RET C634R and RET M918T, with IC50 values of 11.5 nM and 8.3 nM, respectively. It effectively inhibits RET kinase activity and signaling in human thyroid cancer cell lines harboring oncogenic RET alleles, thereby reducing cell proliferation.

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET C634R and RET M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.