(1R)-Deruxtecan is a drug-linker conjugates for ADC[1].
Eclalbasaponin IV is a triterpenoid that can be isolate from the aerial parts of Eclipta prostrata. Eclalbasaponin IV shows antitumor activity in human ovarian cancer cells[1].
Magnoloside B is an α-glucosidase inhibitor (IC50=0.69 mM), which can be obtained from Magnolia officinalis stem bark. Magnoloside B shows moderate inhibitory activity against MGC-803 and HepG2 cells. Magnoloside B has the potential to study cancer and diabetes[1].
GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
Mal-amide-PEG8-Val-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Antitumor agent-100 (compound A6), an apoptosis inducer and molecular glue, shows superior anti-tumor activity[1].
Hydroxygenkwanin (7-O-Methylluteolin), a natural flavonoid compound, is one of the main components of Lilac Daphne. Hydroxygenkwanin has anti-oxidant ability, anti-glioma ability and anticancer effect[1][2].
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2].
NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.
GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
Dalnicastobart (LVGN-7409) is a human IgG1κ antibody targeting CD40/TNFRSF5[1].
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents[1].
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death[1][2][3].
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
Alpinoid D, a diarylheptanoid, can be isolated from the MeOH extract from the rhizomes of Alpinia officinarum Hance. Alpinoid D shows cytotoxic effect against IMR-32 human neuroblastoma cell line[1].
2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM[1][2].
Anticancer agent 52 is a potent anticancer agent. Anticancer agent 52 shows in vitro cytotoxicity. Anticancer agent 52 induces apoptosis. Anticancer agent 52 shows antitumor effect. Anticancer agent 52 has the potential for the research of bladder cancer[1].
Tozasertib is the inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.
Uridine 13C-3 is the 13C labeled Uridine[1].
CSNK1-IN-1 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 21 μM. CSNK1-IN-1 can be used for the research of proliferative disorders[1].
KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
E3 ligase Ligand-Linker Conjugates 33 Hydrochloride incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 33 can be used to design PROTAC degrader[1].
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation[1].
Matrine(Sophocarpidine; α-Matrine) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.IC50 Value: 540 μg/ml (inhibit gastric cancer cell line MNK45, MTT) [1]Target: u-receptor/kappa opioid in vitro: MTT assay showed that the matrine was able to inhibit gastric cancer cell line MNK45 in a dose-dependent manner. The concentration required for 50% inhibition (IC50) was found to be 540 μg/ml. This anti-tumor function was achieved through modulation of the NF-κB, XIAP, CIAP, and p-ERK proteins expression in cell line MNK45. Matrine induces apoptosis of human NSCLC cells with anti-apoptotic factors inhibited and dependent on caspase activity. In addition, we found that matrine increases the phosphorylation of p38 but not its total protein, and inhibition of the p38 pathway with SB202190 partially prevents matrine-induced apoptosis. Furthermore, matrine generates reactive oxygen species (ROS) in a dose- and time-dependent manner, which is reversed by pretreatment with N-acetyl-L-cysteine (NAC) [2].in vivo: Oral administration of matrine (200, 100 and 50 mg/kg) significantly attenuated isoproterenol-induced cardiac necrosis and left ventricular dysfunction [3]. high dose of matrine significantly reduced the mortality rate of mice with LPS administration. Treatment with matrine improved LPS-induced lung histopathologic changes, alleviated pulmonary edema and lung vascular leak, inhibited MPO and MDA activity,and reduced the production of inflammatory mediators including TNF-α, IL-6 and HMGB1 [4].Toxicity: N/AClinical trial: N/A
Modotuximab (Anti-Human EGFR Recombinant Antibody) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab contains a portion of Futuximab that binds to two independent, non-overlapping epitopes on EGFR. Modotuximab promotes cross-linking of EGFR on the cell surface and promotes EGFR cellular internalization and degradation. Modotuximab has antitumor activity in vivo[1].
USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM[1].
N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines[1].
Mifepristone is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
Presenilin 1 (349-361) is an active petide, and synthetic peptides representing amino acids 349–361 can be phosphorylated by glycogen synthase kinase-3β(GSK3β) in vitro. Presenilin 1 (349-361) can be used for the research of various diseases[1].