Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
17-AAG is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90.
Transferrin aldifitox (TF-CRM107) is a diphtheria toxin CRM107 conjugate with transferrin. Transferrin aldifitox can be used to research anticancer[1].
SOS1-IN-13 is a potent son of sevenless homolog 1 (SOS1) inhibitor with IC50s of 6.5 nM and 327 nM for SOS1 and pERK, respectively. SOS1-IN-13 can be used for researching anticancer[1].
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research[1].
Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
OSM-SMI-10B a derivative of OSM-SMI-10. OSM-SMI-10B significantly reduces OSM-induced STAT3 phosphorylation in cancer cells upon co-incubation with OSM (Oncostatin M)[1].
GPX4-IN-5 (Compound C18) is a GPX4 covalent inhibitor with an IC50 value of 0.12 μM. GPX4-IN-5 (Compound C18) can induce ferroptosis for the research of triple-negative breast cancer (TNBC) [1].
3’-O-MOE-A(Bz)-2’-CED-phosphoramidite 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].
Polyethylenimine is a class of cationic polymers, is effective for gene delivery. Polyethylenimine is nondegradable and the molecular weight of PEI affects the cytotoxicity and gene transfer activity. Polyethylenimine acts as a low toxicity and efficient gene vector[1].
Bergapten is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. Bergapten is inhibitory towards mouse and human CYP isoforms.
Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research[1][2].
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer[1].
RCM-1 is a FOXM1 inhibitor.
DB2115 (tertahydrochloride) is a potent inhibitor of myeloid master regulator PU.1. DB2115 (tertahydrochloride) has the potential for the treatment of cancers, including hematologic cancers such as leukemia, as well as other conditions associated with PU. 1 dysfunction (extracted from patent WO2017223260A1, compound DB2115) [1].
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities[1].ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways[2].
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio[1].
CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].
ZIKV-IN-1 is a potent zika virus inhibitor with an EC50 of 2.8 µM and EC90 of 6.8 µM. ZIKV-IN-1 shows anti-ZIKV activity with low cytotoxicity. ZIKV-IN-1 shows a strong affinity to ZIKV RdRp domain[1].
2’-Deoxy-N2,N2-dimethylguanosine 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].
1-NM-PP1 is a cell permeable protein kinase D (PKD) inhibitor with an IC50 of 0.398 μM.
RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
Samalizumab (ALXN 6000) is a humanized monoclonal antibody that specifically binds to CD200 and blocks its ligation to the CD200 receptor (CD200R). Samalizumab can be used for multiple myeloma and B-cell chronic lymphocytic leukemia research[1].
PD153035 (ZM 252868;AG 1517;Tyrphostin AG 1517;SU 5271) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester;Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect[1].
SMCC-DM1 is DM1 with a reactive linker SMCC to make antibody drug conjugate. DM1 (mertansine), a thiol-containing maytansinoid, is a potent microtubule-disrupting agent.
L2H2-6OTD, containing one to four G-quadruplex binding loops, is a telomeric inhibitor analogue. l2H2-6OTD has telomerase inhibitory activity with an IC50 value of 15 nM[1].
Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect[1].
hCAII-IN-1 (compound 7f) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 1.2 and 113.6 nM, respectively. hCAII-IN-1 has the potential for the research of cancer diseases[1].
ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.