Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation[1][2].
Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Uliledlimab is a potent against CD73 humanized monoclonal antibody. Uliledlimab inhibits the conversion of extracellular adenosine monophosphate (AMP) to adenosine. Uliledlimab can be used in research of cancer[1].
2'-epi-2'-O-Acetylthevetin B (GHSC-74) is a cardiac glycoside that can be isolated from the seeds of Cerbera manghas L. 2'-epi-2'-O-Acetylthevetin B inhibits cell viability, induces apoptosis and loss of mitochondrial membrane potential in HepG2 cells[1].
Rohinitib is a potent and specific inhibitor of eIF4A1, inhibits growth and survival of AML cells especially cells with FLT3-ITD.
7,8-Dihydro-8-oxo-7-propargyl-3’-deoxy-3’-fluoro guanosine 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].
Sulfo-SIAB sodium is a nonclaevable monovalent bilinker.
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2[1].
Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata.
Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
Propargyl-PEG4-NHS ester is a nonclaevable 4-unit PEG linker for antibody-drug-conjugation (ADC).
BPR1R024 is an orally active and selective CSF1R inhibitor (IC50 = 0.53 nM).
Antitumor agent-100 hydrochloride (compound A6), an apoptosis inducer and molecular glue, shows superior anti-tumor activity[1].
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
iMDK is a small molecule inhibitor of the growth factor Midkine (MDK) that suppresses the endogenous expression of MDK but not other growth factors such as PTN or VEGF; inhibits the cell growth of MDK-positive H441 lung adenocarcinoma cells that harbor an oncogenic KRAS mutation and H520 squamous cell lung cancer cells, inhibits PI3K pathway and induces apoptosis; significantly inhibits tumor growth in a xenograft mouse model in vivo.
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis[1].
Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
Calcitriol-d3 is the deuterium labeled Calcitriol[1]. Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist[2][3][4][5].
MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape[1].
Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
M3814 is a potent and selective inhibitor of DNA-dependent Protein Kinase (DNA-PK).
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
Benufutamab (GEN1029) is a death receptor 5 (DR5)-specific agonistic antibody. Benufutamab is a mixture of 2 noncompeting DR5-specific IgG1 antibodies, each with an E430G mutation in the Fc domain. Benufutamab has antitumor effects[1].
Azido-PEG4-(CH2)3OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
INO-1001 is a potent and selective Poly (ADP-ribose) polymerase (PARP) inhibitor with an IC50 of 0.05-1 μM. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death[1]. INO-1001 has anti-tumor effects[2].