anti-oncogenic

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.

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.

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.

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Aurothiomalate sodium (Miochrysin) is a potent and selective inhibitor of oncogenic PKC-ι signaling. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium exhibits potent anti-tumor activity.

Aurothiomalate tetramer sodium, a tetrameric form of Aurothiomalate sodium, functions as an anti-arthritis gold agent. It also acts as a potent and selective inhibitor of the oncogenic PKCι signaling pathway.

TRBP-IN-1 (Compound 13j) is an orally active inhibitor of TAR RNA-binding protein 2 (TRBP) with an IC50 of 12.72 μM. It exhibits significant anti-hepatocellular carcinoma (HCC) activity, effectively suppressing proliferation and metastasis of HCC cells [HCCLM3 cells (IC50: 18.96 μM) and SK-Hep-1 cells (IC50: 16.45 μM)]. TRBP-IN-1 modulates miRNA biosynthesis by targeting TRBP, inhibiting the expression of oncogenic miRNAs. It induces apoptosis and pyroptosis in HCC cells by decreasing miRNA levels. TRBP-IN-1 is suitable for research on targeted HCC therapy.

Prmt5-IN-20 chloride is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor. It strongly disrupts the activation of oncogenic transcriptional programs by blocking the symmetric dimethylation of histone and non-histone proteins, exhibiting outstanding anti-proliferative activity in various hematological and solid tumor models.

Dibrospidium Free Base is a dispirotripiperazine derivative and alkylating agent with potential antineoplastic and anti-inflammatory activities. The duration of DNA synthesis inhibition in tumor cells was found to correlate with spirobromine antitumor activity. Spirobromin is superior to prospidin by the power of the anti-inflammatory effect. Spyrobromin can diminish the latent period of the development of tumours in the experimental rats at intraperitoneal administration. At intragastric administration of the drug no decrease was noted in the latent period and no increase of tumours was observed in the experimental groups of the animals as compared with control. Dibrospidium has been examined for the treatment of bone cancer. The oral route of administration is the most safe with respect to the oncogenic risk. It was noted that spirobromin exerted the most pronounced toxic action on erythrocytes. Dibrospidium is used for the treatment of acute leukemias (mainly in combinatio......

1. Demethoxycurcumin (Desmethoxycurcumin) has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.

KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ).

HSP70-IN-3, a potent inhibitor of HSP70 with IC50 values of 1.1 μM in ASZ001 cells and 1.9 μM in C3H10T1/2 cells, exhibits anti-Hedgehog (Hh) signaling and anti-proliferative activities. Furthermore, it reduces the expression of the oncogenic transcription factor GLI1 [1].

Genkwadaphnin, a daphnane diterpenoid, targets importin-β1, reducing the nuclear accumulation of CRPC drivers and suppressing downstream oncogenic signaling. Demonstrating potent anti-tumor effects, it inhibits castration-resistant prostate cancer (CRPC) in vivo in mice [1].

Anti-F3/Factor III/Tissue Factor/CD142 Antibody represents a highly specialized monoclonal antibody specifically engineered to target the human Tissue Factor (TF/CD142) with exceptional binding affinity. It effectively facilitates the measurable targeting of TF-expressing malignant cells across various preclinical experimental models to evaluate the delivery of cytotoxic payloads or the disruption of TF-mediated oncogenic signaling during strictly monitored laboratory observation periods and functional cell viability assays without compromising systemic coagulation homeostasis.

Anti-ERG Antibody is a highly specialized monoclonal antibody target the human ETS-related gene protein, which serves as a definitive transcription factor marker for vascular endothelial cells and is frequently overexpressed in prostate malignancies due to chromosomal translocations, detection of ERG-positive cellular populations across various preclinical experimental models to study oncogenic signaling pathways and the molecular mechanisms of neoplastic transformation in glandular tissues.

Anti-CDCP1/CD318 Antibody (38 E11) is a potent monoclonal antibody targeting the extracellular domain of the transmembrane glycoprotein CDCP1, acting by specifically binding to its CUB1 domain. The compound is an essential tool for investigating Src-dependent signaling, tumor cell survival, and distal metastasis mechanisms, aiming to downregulate downstream oncogenic signaling cascades by blocking CDCP1 phosphorylation or inducing its internalization.

MM-111 is a bispecific antibody fusion protein targeting the oncogenic units ErbB2/ErbB3. It obstructs the activation of the PI3K survival pathway. By binding to the ErbB2 receptor, MM-111 localizes the bispecific molecule to ErbB2-overexpressing tumor cells, facilitating the interaction of its anti-ErbB3 arm with the ErbB3 receptor. This binding inhibites ErbB3 signaling by preventing the ErbB3 receptor from associating with its physiological ligand, heregulin. MM-111 is applicable in the study of ErbB2-overexpressing breast tumors.

AG01 is a monoclonal antibody targeting the anti-granular protein precursor (GP88). It inhibits the proliferation and migration of triple-negative breast cancer (TNBC) cells, reducing the expression of phosphorylated protein kinases such as p-Src, p-AKT, and p-ERK, as well as oncogenic proteins like Axl, c-MET, HIF-1α, and VEGF. In TNBC xenograft mouse models, AG01 suppresses tumor growth and the expression of Ki67 in vivo. AG01 is useful for research involving cancers like TNBC.

Demethoxy Curcumin-D4 is a deuterated compound of Demethoxy Curcumin. Demethoxy Curcumin (T6S1683) has a CAS number of 22608-11-3. 1. Demethoxycurcumin has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.

Demethoxycurcumin (Standard) is a reference standard for research and analysis in studies involving Demethoxycurcumin. 1. Demethoxycurcumin (Desmethoxycurcumin) has antioxidant activity. 2. Demethoxycurcumin has anti-inflammatory activity. 3. Demethoxycurcumin has anti-proliferative activity. 4. Demethoxycurcumin has anti-acanthamoebic effect. 5. Demethoxycurcumin is a potential additive natural product in combination with chemotherapeutic agents in drug-resistant cancers. 6. Demethoxycurcumin inhibits energy metabolic and oncogenic signaling pathways through AMPK activation in triple-negative breast cancer cells.