Cancer Targeted Therapy

1-(2,3-Dideoxy-β-D-erythro-hexo pyranosyl)cytosine 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.

Tos-PEG7-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Apolizumab (Hu1D10) is a humanized monoclonal anti-Human leukocyte antigen-DR beta-chain antibody. Apolizumab can mediate apoptosis of chronic lymphocytic leukemia (CLL) cells in vitro.

FTO-IN-2 is a FTO inhibitor that impairs self-renewal in glioblastoma stem cells.

HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer.

CPP-13 is a selective PARP1 PROTAC degrader with a DC₅₀ of 0.48 nM. CPP-13 induces CRBN-dependent ubiquitination and proteasomal degradation of PARP1. CPP-13 induces DNA damage. CPP-13 inhibits the growth of BRCA-deficient breast cancer and pancreatic cancer. CPP-13 can be used in studies related to BRCA-deficient breast cancer and BRCA-deficient pancreatic cancer.

Z-VDVA-(DL-Asp)-FMK is a Z-VDVAD-FMK derivative. Z-VDVAD-FMK (HY-P1008) is a special inhibitor of caspase-2.

GNR-051 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. GNR-051 can be used in Solid tumours research.

hsa-miR-3661 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.

CDK2/4-IN-2 (compound 56) is a CDK2 and CDK4 dual inhibitor with IC₅₀s less than 100 nM. CDK2/4-IN-2 can be used in the study of cancer.

HDAC6 ligand-4 is a targeted ligand for histone deacetylase 6 (HDAC6). HDAC6 ligand-4 can serve as a target protein ligand for TO-1187 (HY-173266) and is used in studies related to PROTAC synthesis.

Fmoc-Val-Cit-PAB-Exatecan is a Drug-linker conjugate for ADC. Fmoc-Val-Cit-PAB-Exatecan contains the ADC linker (Fmoc-Val-Cit-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).

MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC₅₀ values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia.

Allopole-A is a Plk1 inhibitor with an IC₅₀ of 1.4-2.5 μM against human Plk1 PBD1. Allopole-A binds to the allosteric W-F pocket in Plk1 PBD1, displacing the L2 loop, thereby disrupting water-mediated phospho-ligand binding interactions and promoting inhibitory interactions between the kinase domain and PBD to suppress Plk1 kinase activity. Allopole-A can be used in studies of human cancers with plk1 overexpression.

1,2-Dimethylpyridinium iodide-Bodipy (Probe 1) is an H₂S fluorescent probe. Self-assembled 1,2-Dimethylpyridinium iodide-Bodipy exhibits highly efficient responsiveness to H₂S. The assembled form of 1,2-Dimethylpyridinium iodide-Bodipy emits near-infrared fluorescence at 718 nm upon H₂S activation.

Echinoside A is a saponin. Echinoside A can be isolated from sea cucumber. Echinoside A inhibits the catalytic activity of Top2α, reduces the noncovalent binding of Top2α to DNA. Echinoside A activates Caspase-3 and induces PARP cleavage. Echinoside A induces Apoptosis. Echinoside A has anticancer activity against prostate cancer, hepatocellular carcinoma, and S-180 sarcoma. Echinoside A exhibits antifungal activity against a variety of fungi, with a minimum growth inhibitory concentration range of 3.12 to 50.0 μg/mL, including potent activity against Aspergillus and Penicillium species.

[D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is a potent inhibitor of cell growth in small cell lung cancer (SCLC). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P is also a neuropeptide antagonist, capable of blocking colony formation stimulated by various neuropeptides (including vasopressin and bradykinin). [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the mobilization of Ca²⁺ and the activation of mitogen-activated protein kinases induced by vasopressin or bradykinin. [D-Arg1, D-Trp5, 7, 9, Leu11]-Substance P inhibits the growth of H-69 xenograft tumors in nude mice.

hsa-miR-148b-3p 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.

Biotin-PEG5-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.