Cancer Targeted Therapy

IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC₅₀: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.

TGF-βR1/VEGFR2-IN-1 is a dual inhibitor targeting TGF-βR1/VEGFR2, with an IC₅₀ of 232.5 nM against human TGF-βR1 and an IC₅₀ of 371.4 nM against human VEGFR2. TGF-βR1/VEGFR2-IN-1 mediates antiproliferative effects by inhibiting the TGF-βR1 and VEGFR2 signaling pathways. TGF-βR1/VEGFR2-IN-1 can be used in research related to colorectal cancer, non-small cell lung cancer, cervical cancer, and hepatocellular carcinoma.

8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility.

WEE1-IN-12 (Compound 87) is a Wee1 kinase inhibitor with an IC₅₀ of 2.0 nM. WEE1-IN-12 can inhibit the proliferation of HT29 cells (IC₅₀: 1.07 μM), and when used in combination with Gemcitabine (HY-17026), the effect is better (IC₅₀: 0.34 μM). WEE1-IN-12 can be used in the research of tumors such as colon cancer.

mPGES1-IN-10 (Compound 7d) is a potent microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor with an IC₅₀ value of 1.0 μM. mPGES1-IN-10 is promising for research of chronic inflammation-related diseases and malignancies such as colorectal cancer.

PLX-4104 is an orally active BRD4 molecular glue degrader with a DC₅₀ of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia.

MC-PSE is a fluorescent probe that can be used for glutathione (GSH) detection, NIR-II fluorescence imaging and ratiometric photoacoustic imaging. MC-PSE spontaneously forms J-aggregates in aqueous solution through π-π stacking, and its phenylselenyl group acts as a fluorescence quencher and GSH recognition receptor, thereby eliminating intrinsic fluorescence and generating a maximum absorption peak at 1000 nm. The excitation/emission wavelengths of MC-PSE are Ex = 808 nm and Em = 940 nm. MC-PSE can be applied in tumor-related research.

hsa-miR-4660 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.

hsa-miR-604 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.

hsa-miR-8065 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.

mmu-miR-350-5p 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.

mmu-miR-6986-3p 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.

rno-miR-295-3p 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.

Propargyl-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG3-Boc is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC₅₀ values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC₅₀ of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity.

Fimepinostat mesylate 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.

Thalidomide-NH-C2-2-azaspiro[3.3]heptane is a conjugate of E3 ubiquitin ligase ligand + Linker, used for the synthesis of KT-413 (HY-153368).

WRN inhibitor 18 (compound 306) is an orally available inhibitor of WRN with in vivo anticancer activity.

HYNIC-iPSMA is a PSMA-targeted ligand for tumor molecular imaging, with a K_i value of 3.11 nM. HYNIC-iPSMA consists of two components: HYNIC (6-hydrazinonicotinamide) and iPSMA (Inhibitor of Prostate-Specific Membrane Antigen). HYNIC acts as a chelating moiety to link radionuclides to the targeting molecule; iPSMA is a specific inhibitor that targets Prostate-Specific Membrane Antigen (PSMA). 68Ga-labeled iPSMA is used for prostate cancer detection via PET imaging, while the further developed ^99mTc-EDDA/HYNIC-iPSMA TFA exhibits excellent specificity and sensitivity. HYNIC-iPSMA can be used for the synthesis and research of radionuclide-conjugated drugs (RDC).

hsa-miR-298 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.