Zimberelimab is a fully human IgG4 anti-PD-1 monoclonal antibody with high affinity and selectivity. Zimberelimab shows antitumor activities and can be used for various cancers research including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma[1].
RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered.
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research[1].
Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM.
SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research[1].
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
1-O-Acetyl-2-O-benzoyl-3-O-tert-butyldiphenylsilyl-L-threofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation[1][2][3][4].
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2, respectively. JAMM protein inhibitor 2 can be used for researching anticancer[1]
N6-Bz-5’-O-DMTr-2’-O-hexadecanyl adenosine 3’-CED phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
Berteroin, a naturally occurring Sulforaphane analog, ia an antimetastatic agent. Berteroin has anti-inflammatory, antitumor and bactericidal effects[1][2].
CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities[1].
Davelizomib is proteasome inhibitor with antineoplastic effect[1].
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
Moracin O is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin O exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects[1][2][3].
Ro 5126766 is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC50 of 0.15 nM. NSC81111 has anticaner effects[1].
KRAS G12C inhibitor 46 (compound WX003) is a potent KRAS G12C inhibitor[1].
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
RET-IN-10 is a potent inhibitor of RET. RET loss of function mutations leads to Hirschsprung's disease, while its gain of function mutations is associated with a variety of human tumors. RET-IN-10 has the potential for the research of cancer diseases (extracted from patent WO2021135938A1, compound 18)[1].
CDK7-IN-21 (compound A22) is a potent CDK7 inhibitor[1].
CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer[1].
Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays.
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity[1][2].
Ragifilimab (INCAGN-1876) is an agonist monoclonal antibody targeting the glucocorticoid-induced TNFR-related protein (GITR). Ragifilimab can be used for advanced or metastatic solid tumors research[1].
CGP60474 is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM, and also an ATP-competitive PKC inhibitor.