Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523)[1].
Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1]. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways[2].
Bromo-PEG2-acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
XmAb 5592 is a humanized, Fc-engineered anti-HM1.24 antibody with enhanced binding to FcγRIIIa and FcγRIIa receptors, augments HM1.24-specific multiple myeloma (MM) cells lysis in vitro via antibody-dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP)[1].
Phosphatase Binder-1 (comppund i-196) provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Phosphatase Binder-1 plays an important role in cancer[1].
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44)[1].
Jaceidin is a promising lead molecule for potent VEGFR inhibitor with excellent membrane permeability and oral bioavailability. Jaceidin exhibits anti-tumor activities[1].
CDK2-IN-15 (Compound 19) is an inhibitor of CDK2 with an IC50 of 2.9 μM. CDK2-IN-15 can be used for cancer research[1].
(S)-GFB-12811 (compound 596) is a potent and selective CDK5 inhibitor, with an IC50 value less than 10 nM. (S)-GFB-12811 can be used in the research of cell cycle progression, neuronal development, tumorigenesis[1].
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.
(32-Carbonyl)-RMC-5552 is a potent mTOR inhibitor. (32-Carbonyl)-RMC-5552 inhibits mTORC1 and mTORC2 substrate (p-P70S6K-(T389), p-4E-BP1-(T37/36), AND p-AKT1/2/3-(S473)) phosphorylation with pIC50s of > 9, >9 and between 8 and 9, respectively (patent WO2019212990A1, example 2)[1].
3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
2',5'-Bis-O-(triphenylMethyl)uridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
Testololactone is an aromatase inhibitor. Testololactone can be used for research of breast carcinoma[1].
Eftilagimod alfa (IMP321) is a recombinant LAG-3Ig fusion protein that binds to MHC class II. Eftilagimod alfa mediates antigen-presenting cell (APC) activation followed by CD8 T-cell activation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research[1].
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease[1].
ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.IC50 Value: Target: DYRKin vitro: the combination of Wnt and ID-8 enhanced hESC replating efficiency, and colonies expressed ALP and displayed undifferentiated morphology. members of the DYRK family are direct targets of ID-8 and that ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs [1]. ID-8 stimulated proliferation at a steady rate similar to LIF. ID-8 is required to maintain nanog, Sox2, and Rex-1 gene expression [2]. In vivo:
OSU-03012 is a PDK-1 inhibitor with an IC50 of 5 μM.
Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.
Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects[1][2][3].
Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research[1].
m-PEG5-triethoxysilane is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Sophocarpine (monohydrate) 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 (monohydrate) 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 (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities[1].
Teneliximab (BMS-224819) is a chimeric monoclonal antibody, blocks the CD40-CD40L interaction. Teneliximab (BMS-224819) has partial agonist activity resulting in some signaling through CD40 and peripheral B cell depletion[1].
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
Zoledronic Acid is a third-generation, nitrogen-containing bisphosphonate, inhibits osteoclast-mediated bone resorption, and also has antitumor activity.