XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
Canertinib dihydrochloride (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
(S,R,S)-AHPC-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology[1].
MDL-800 is an activator of SIRT6 deacetylation, with an EC50 value of 10.3 µM[1].
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect[1][2][3].
L-Cystine N-carboxyanhydride can be used for synthesis of polyamino acid carrier for anti-tumor agent delivery[1].
BocNH-PEG5-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TAK-448 acetate (MVT-602 acetate) is a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM[1].
Biotin-PEG5-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
Galiximab (IDEC 114) is a primatized immunoglobulin G1 (IgG1) lambda monoclonal antibody directed against the CD80 antigen. Galiximab has variable regions are primatized (cynomologous monkeys), and the constant regions are human. Galiximab can be used in research of B-cell lymphoma[1].
CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM)[1]. CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis[2].
Tetramethylrhodamine-5-isothiocyanate is a potent fluorescent dye. Tetramethylrhodamine-5-isothiocyanate can be used for label PG-M3 antibody for rapid diagnosis of acute promyelocytic leukemia (APL). Tetramethylrhodamine-5-isothiocyanate can be used as probe to quantify in vivo the biodistribution of PLGA (poly(lactic-co-glycolic) acid) and PLGA/chitosan nanoparticles[1][2].
ER degrader 6 (compound 35s) is a potent Estrogen Receptor (ER)α degrader. ER degrader 6 disrupts the microtubule network by restraining tubulin polymerization. ER degrader 6 suppresses tumor growth without noticeable poisonousness[1].
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes[1].Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner[2]. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis[3].
MRX-2843 is an orally available small-molecule inhibitor of both MERTK and FLT3.
KP-23172 is a PI3-K/Akt pathway inhibitor extracted from patent US7196083[1].
BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK 9 kinases.
Isobavachalcone(Corylifolinin) is a chalcone constituent of Angelica keiskei, induces apoptosis in neuroblastoma.IC50 value:Target: Isobavachalcone inhibits platelet aggregation. Inhibitor of Epstein-Barr virus early antigen (EBV-EA) induction. Isobavachalcone exhibits potent inhibitory effect on skin tumor promotion. Potent inhibitor of MMP-2. Displays DNA strand-scission (cleaving) activity. Isobavachalcone hows antifungal activity.
5'-DMTr-2,2'-anhydrothymidine 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].
Vonlerolizumab (MOXR 0916) is a humanized IgG agonistic monoclonal OX40-specific antibody. Vonlerolizumab can be used for the research of cancer[1].
IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
MTL-CEPBA is a small activating RNA targeting for upregulation of C/EBPα. MTL-CEPBA has anti-inflammatory and anti-cancer activity[1].
Dehydrobruceantin has potential antileukemic activity[1].
A small-molecule partial agonist of CXCR7 (ACKR3).
6-shogaol, an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
Trifluridine is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection.
AP1867-3-(Methoxyethylamine), the AP1867 based moiety, is a synthetic ligand for FKBP. AP1867-3-(Methoxyethylamine) can be used in the synthesis of PROTAC FKBP12 F36V degrader[1].
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV[1].
USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.