cancer cell

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.

Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure.

NNK is a nitrosated derivative of nicotine that activates the ERK1/2 and PKCα signaling pathways, induces Bcl2 phosphorylation at Ser70, and activates c-Myc at Thr58 and Ser62, thereby promoting the proliferation and survival of human lung cancer cells, and is commonly used to establish lung cancer mouse models.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Cyclic-di-GMP disodium (5GP-5GP disodium) is a STING agonist and a second messenger in bacteria. It is involved in a variety of processes in prokaryotes, including biofilm formation, motility, and cell cycle progression. Cyclic-di-GMP disodium (5GP-5GP disodium) exhibits antiproliferative activity against cancer cells, inducing increased CD4 receptor expression and cell cycle arrest, and is a novel therapeutic agent that can be developed to prevent or treat cancer.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

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.

MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.

Nivolumab is a monoclonal antibody and is a humanized PD-1 antibody. Nivolumab has anti-tumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma, etc.

Divarasib (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.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R/T790M mutant non-small cell lung cancer.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

DIQ3 is non-toxic to normal human cell lines and is an effective anti-cancer agent.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

KRAS G12C inhibitor 16 is a potent inhibitor of KRAS G12C.

LB-60-OF61 is a NAMPT inhibitor that exhibits antiproliferative activity against MYC oncogene-dependent cancer cell lines (brackets).

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).