Cancer Targeted Therapy

hsa-miR-1269a antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

IAJD-97 is a single-component ionizable amphiphilic Janus dendrimer carrier targeting mRNA delivery, which self-assembles into dendrimersomes (DNPs) via pH-responsive mechanisms to efficiently encapsulate and protect mRNA, while facilitating cellular uptake and endosomal escape through ionizable amine groups. IAJD-97 is promising for research of cancers.

Boc-NH-PEG15-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

4,7-Dihydroxycoumarin is an EGFR inhibitor, estrogen receptor inhibitor, and progesterone receptor inhibitor. 4,7-Dihydroxycoumarin against breast cancer cells with an IC₅₀ velue of 18.36 μg/mL. 4,7-Dihydroxycoumarin can be used for the research of breast cancer.

hsa-miR-429 inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC₅₀ of 26.3 μM.

Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (K_A = 2 x 10⁵ /M) and thereby increases the length of linear DNA.

Xanthomicrol is extracted from the resin of the plant called Chinese bellflower (a member of the Scrophulariaceae family) and is a monoamine oxidase (MAOs) inhibitor. Xanthomicrol has anti-tumor and anti-inflammatory properties, with IC₅₀ values of 0.88 and 1.69 μg/mL in HL60 and K562 cells. Xanthomicrol's the main metabolite of 5DT in mouse colon, and it can reduce levels of iNOS protein and mRNA, as well as COX-2 protein levels. Additionally, Xanthomicrol decreases the production of the pro-inflammatory cytokine IL-1β and induces the expression of the antioxidant enzyme HO-1.

Azaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC₅₀ values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections.

PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC₅₀ of 14.2 nM against BRD4 BD1.

Lapiteronel (CFG920) is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. Lapiteronel has the potential for metastatic castration-resistant prostate cancer research.

S3I-1757 is a STAT3 inhibitor. S3I-1757 inhibits the phosphorylation and dimerization of STAT3. S3I-1757 can be used for the research of STAT3 hyperactive cancers such as melanoma.

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC₅₀ of approximately 5.86 μM at 24 h.

Evernic Acid is an orally active thioredoxin reductase 1 (TrxR1) inhibitor and antiproliferative agent. Evernic Acid inhibits the proliferation and migration of human breast cancer cells. Evernic Acid blocks the NF-κB pathway by inhibiting p65 nuclear translocation and IκBα phosphorylation, thereby suppressing downstream inflammatory mediators. Evernic Acid acts as an antioxidant, anti-inflammatory agent and neuroprotective agent, protects neurons from cell death, mitochondrial dysfunction and oxidative stress damage, reduces astrocyte activation, and ameliorates dopaminergic neuron loss and neuroinflammation. Evernic Acid inhibits enoyl reductases FabI and FabZ of Plasmodium falciparum. Evernic Acid downregulates the expression of lasB and rhlA genes in Pseudomonas aeruginosa, inhibits quorum sensing and biofilm formation, and exerts antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and fungi. Evernic Acid is applicable to research related to breast cancer, Parkinson's disease, bacterial infections and fungal infections.

MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan is a pharmaceutical composition containing antibody agent conjugate (ADC). (extracted from patent WO2021190581 Example 1-8).

Dehydromonocrotaline is a mitochondrial respiratory chain complex I NADH oxidase inhibitor, with a IC₅₀ of 62.06 μM and a K_i of 8.1 μM in rats. Dehydromonocrotaline exerts non-competitive inhibitory effects by modifying cysteine thiol groups on complex I, and does not bind to the NADH-binding site. Dehydromonocrotaline dissipates mitochondrial membrane potential and reduces ATP levels. Dehydromonocrotaline can be used in studies related to hepatotoxicity, pulmonary hypertension and liver tumors.

LXY3 (LXY2) is a VLA-3-blocking peptide that inhibits the interaction between integrin α3β1 (VLA-3) on neutrophil surfaces and laminin in the basement membrane, thereby preventing neutrophil migration across the tumor vascular basement membrane barrier. LXY3 is used to block neutrophil-mediated nanoparticle release from perivascular pools into the tumor interstitium. LXY3 is commonly employed for targeted imaging of breast cancer.

NRP1 antagonist 2 (Compound 1) is an NRP1 antagonist.

(R)-Glutor is the R-enantiomer of Glutor (HY-158302). Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.