Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells[1].
epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits ERK1/2 and JNK activation, which suppresses Bcl-2 expression[1].
Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
Thalidomide-Piperazine 5-fluoride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Dibenzo(a,i)pyrene is a 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) receptor ligand[1].
Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo[1].
Monomethyl auristatin E intermediate-12 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC50 value of 28.58 μM[1].
Luteolin is a falconoid compound, which exhibits anticancer properties.IC50 value:Target: A natural for anticancer.In vitro: Luteolin exerted an anticancer effect against NCI-H460 cells through Sirt1-mediated apoptosis and the inhibition of cell migration [1]. The treatment of luteolin upregulated the expression levels of transforming growth factor β1 (TGF-β1), p21WAF1/CIP1, p27KIP1, Smad4, and Fas in HCC cells. Luteolin induced apoptotic cell death in Hep3B cells while caused G1 arrest in HepG2 cells. And it induces apoptosis from G1 arrest via three signaling pathways of TGF-β1, p53, and Fas/Fas-ligand in HCC cells [2].In vivo: The study of the effect of Luteolin on the improvement of cancerous cachexia in model mice showed that luteolin can improve the symptoms of cancer cachexia model mice.The mechanism may be related to inhibition of proteasome and calcium activated protease activity and lower the levels of cytokines [3].
Menin-MLL inhibitor 24 (compound A) oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor, and can be used for the research of cancer[1].
Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells[1].
ATG7-IN-2 (compound 1) is a potent ATG7 inhibitor, with an IC50 of 0.089 μM. ATG7-IN-2 inhibits autophagy marker LC3B[1].
CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.
Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells[1].
Momordicoside L is a Cucurbitane Triterpenoid, that can be isolated from the leaves of Momordica charantia. Momordicoside L shows anticancer activity[1].
SHMT-IN-1 (compound (±)-46) is a potent inhibitor of plasmodial serine hydroxymethyltransferase (SHMT). SHMT-IN-1 has antitumor activity[1].
Vepsitamab (AMG 199) is an anti-MUC17/CD3 BiTE antibody that binds to CD3 on T cells and MUC17 expressed on tumor cells, mediates redirected tumor cell lysis, and induces T cell activation and proliferation[1].
Forodesine hydrochloride is a potent and oral purine nucleoside phosphorylase (PNP) inhibitor with IC50s ranging from 0.48 to 1.57 nM.
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
Nitromifene is an antagonist of estrogen receptor (ER).
EZH2-IN-3 is a highly selective small molecule inhibitor of EZH2 and EZH1 with IC50 of 21/197/213 nM for wt EZH2/EZH2 Y641N/wt EZH1 respectively; suppresses global histone H3-lysine 27 methylation and cause selective proliferation defects.
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity[1]. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1)[2]. Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes[3].
Heveaflavone is an anticancer and antioxidant agent[1].
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family[1][2][3].
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
SIRT2-IN-11 (AEM1) is a selective SIRT2 inhibitor with an IC50 value of 18.5 μM. SIRT2-IN-11 p53-dependently induces apoptosis, activates expression of CDKN1A, PUMA and NOXA, and increases acetylation of p53. SIRT2-IN-11 can be used for the research of p53-related cancers[1].
ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM)[1].
GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration.3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg.4) GNF-6231 showed very robust dose-related antitumor efficacy.
MK-8353 is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
Sotigalimab, a CD40 agonistic monoclonal antibody, can be used for the research of metastatic pancreatic adenocarcinoma[1].