Pasakbumin D is a quassinoid and can be used for the research of cancer[1].
MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). MAT2A inhibitor 4 can be used for the research of cancer[1].
4A3-SC8 is a modular degradable dendrimer that enables small RNAs to extend survival in an aggressive liver cancer model[1].
EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1[1].
Mini Gastrin I, human is a shorter version of human gastrin 1, consists of amino acids 5-17 of the parent peptide, and binds with the CCK2i4svR.
AEEA-AEEA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). AEEA-AEEA is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
Mal-PEG4-VA-PBD is a drug-linker conjugate for ADC by using the antitumor antibiotic, Pyrrolobenzodiazepine (PBD), linked via Mal-PEG4-VA.
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM[1].
Hemiasterlin ((-)-Hemiasterlin) is an antimitotic marine natural product with potent anticancer effcts. Hemiasterlin can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs)[1].
PI3Kδ-IN-15 (compound 6b) is a selective PI3Kδ inhibitor with an IC50 of 0.5 nM for p110δ. PI3Kδ-IN-15 inhibits PI3Kδ with >30-fold higher potency than PI3Kγ, PI3Kβ, and PI3Kα[1].
RS5517 is a specific PDZ1-domain antagonist of NHERF1 that prevented its ectopic nuclear entry. RS5517 can be used for the research of colorectal cancer[1][2].
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
Ivonescimab (AK112) is a PD-1/VEGF Bispecific Antibody. Ivonescimab can be used for cancer research[1][2][3].
MC-GGFG-NH-CH2-O-CH2-(s-cyclopropane)-COOH is an ADC linker that can be combined with the cytotoxic Camptothecin (HY-16560) to form an ADC-related drug-linker conjugate (Drug- Linker Conjugates for ADC).MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is conjugated to Camptothecin, which can further bind to the antibody Trastuzumab (HY-P9907) to form Antibody-Drug Conjugates (ADCs)[1].
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase[1].
L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK)[1]. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[2].
Triamcinolone Acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone. Target: Glucocorticoid ReceptorTriamcinolone acetonide is a synthetic corticosteroid used to treat various skin conditions, to relieve the discomfort of mouth sores, and in nasal spray form, to treat allergic rhinitis. It is a more potent derivative of triamcinolone, and is about 8 times as potent as prednisone [1].
NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.
JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).IC50 value: 4.8 nM [1]Target: JAK3in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1]in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng·h/mL following a 10 mg/kg oral dose and good oralbioavailability of 66%. [1]
(S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis[1].
TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition[1].
DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM.
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1].
TPEN is a specific cell-permeable heavy metal chelator.
E7820 is an angiogenesis inhibitor by suppressing integrin a2, a cell adhesion molecule expressed on endothelial cells.
VEGFR-2-IN-20 (Compound 7) is a potent inhibitor of VEGFR. VEGFR-2-IN-20 has the potential for the research of cancer diseases[1].
Tolfenamic acid-13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
10α-Hydroxyepigambogic acid can be extracted from Garcinia hanburyi. 10α-Hydroxyepigambogic acid can be used in the research of tumors[1].