cell growth

Galloflavin is a lactate dehydrogenase inhibitor that inhibits the activity of lactate dehydrogenase. Galloflavin inhibits both human LDH isoforms (type A and type B) by preferentially binding to the free enzyme without competing with substrates or cofactors, with Ki values ​​calculated by pyruvate of 5.46 μM (LDH-A) and 15.06 μM (LDH-B).

BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.BI-2493 exhibits antitumor activity and inhibits tumor cell growth and can be used in the study of cancerous diseases.BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.

PND-1186 (VS-4718) is a specific and reversible FAK inhibitor with an IC50 of 1.5 nM.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRβ, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

DI-87 (TRE-515) is a novel and orally available dCK (deoxycytidine kinase) inhibitor with good in vitro activity and low protein binding. DI-87 binds to dCK and prevents the phosphorylation of deoxycytidine by dCK, which reduces the production of dNTP and cell cycle arrest (especially in S phase). When combined with thymidine, DI-87 significantly inhibits tumor growth.

Datopotamab deruxtecan (DS-1062) is a trophoblast cell surface antigen 2 (TROP2)-targeted antibody-drug conjugate (ADC) with antitumor activity. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

GA-017 is a potent, selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1 2), exhibiting IC50 values of 4.10 and 3.92 nM, respectively. This compound simultaneously acts as an activator of cell proliferation by promoting YAP TAZ activation and their nuclear translocation. Additionally, GA-017 enhances cell growth in 3D culture conditions and augments the ex vivo formation of mouse intestinal organoids [1].

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.

Adhesamine, a dumbbell-shaped molecule, plays a crucial role in activating the MAPK FAK pathway, thus promoting mammalian cell adhesion and growth. Additionally, it accelerates the differentiation and enhances the survival of mice hippocampal neurons in primary culture.

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

Bevacizumab, a humanized monoclonal antibody, specifically and with high affinity binds to all isoforms of VEGF-A.

Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis.

Divarasib (GDC-6036) (GDC-6036) is an investigational, oral, high-potency and selective KRAS G12C inhibitor with an IC50 of < 0.01 μM. Divarasib irreversibly locks KRAS G12C oncoprotein in an inactive state and inhibits tumor cell growth. It is being investigated for use in solid tumors, including non-small cell lung and colorectal cancers and other types of cancer.

K-80003(TX-803) is a potent retinol-like X-receptor-alpha regulator that inhibits TRxrα-dependent Akt activation and tumor cell growth.

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

Sabizabulin (ABI-231) is a potent, orally bioavailable α- and β-tubulin inhibitor that is active against melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells by targeting HPV E6 and E7 and is also being studied in prostate cancer.

CID-663143 inhibits cancer cell growth and shows microtubule-binding activity.

CLK1 2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1 2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.

CT-2584 is an anticancer agent that inhibits phospholipid signaling and kills tumor cells through the production of reactive oxygen intermediates. CT-2584 reduces NKEF-B expression in several tumor cell types. CT-2584 reduced tumor growth in SCID mice by causing shunting of ab initio phospholipid biosynthesis from phosphatidylcholine (PC) to phosphatidylinositol (PI) via PA.

ND-322 HCl (ND 322 Hydrochloride) is a selective inhibitor of MT1-MMP and MMP2 and reduces in vitro melanoma cell growth, migration and invasion.