Cancer Targeted Therapy

mmu-miR-8106 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.

H-Tyr-Phe-OH-¹³C₉,¹⁵N ( (L-Tyrosyl-L-phenylalanine-¹³C₉,¹⁵N)) TFA is the ¹³C- and ¹⁵N-labeled H-Tyr-Phe-OH (HY-W011258). H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells.

KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC₅₀s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers.

hsa-miR-1298-5p 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.

mmu-miR-1195 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.

Amino-PEG10-OH is non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG10-OH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

THP-PEG1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity.

Trifluridine-¹³C,¹⁵N₂ is the ¹³C and ¹⁵N labeled Trifluridine. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity.

Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET R749T is a mutant of RET. RET R749T Recombinant Human Active Protein Kinase is a recombinant RET R749T protein that can be used to study RET R749T-related functions.

IGN-786 Antibody is an antibody that targets the leukemia anti-surface antigen (SAIL). IGN-786 Antibody can be used to synthesize the ADC molecule IGN-786. IGN-786 Antibody can be used in leukemia-related research.

Gedatolisib-d₆ (PKI-587-d₆) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.

8-Benzyloxy-3’-deoxy-3’-fluoroguanosine 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.

TPP-Ce6 is a mitochondria-targeted photosensitizer formed by the ester bond conjugation of chlorophyll e6 (Ce6) with triphenylphosphine (TPP). Under light irradiation or ultrasound exposure, TPP-Ce6 generates reactive oxygen species, induces cell apoptosis, and triggers immunogenic cell death. TPP-Ce6 can serve as a component of carrier-free co-delivery systems, undergo enzyme-induced self-assembly within tumors, and modulate tumor hypoxia. TPP-Ce6 is applicable to research on breast cancer and glioblastoma.

FLT3-IN-25 (compound 17) is a potent inhibitor of FLT3, with IC₅₀s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML).

Hyp-dBET1 is a hypoxia-activated BRD4 PROTAC degrader. The IC₅₀ of Hyp-dBET1 for reducing cell viability under hypoxic conditions is approximately 153 nM to 192 nM, while it shows low activity under normoxic conditions (IC₅₀ of approximately 2.8 μM to 3.8 μM). Hyp-dBET1 induces BRD4 degradation under hypoxic conditions, converts to dBET1 in hypoxic environments, and downregulates the expression level of ZFP-91. Hyp-dBET1 can be used in studies related to breast cancer, cervical cancer and solid tumors.

RAF-IN-2 is a RAF inhibitor. RAF-IN-2 can be used for proliferative diseases such as leukemia, psoriasis and fibrosis research.

ULK1/2-IN-1 is a tissue-targeted ULK1/2 inhibitor conjugated to the RGR (CRGRRST) tumor neovasculature-homing peptide. ULK1/2-IN-1 mediates autophagy inhibition and induces cytotoxicity in endothelial cells. ULK1/2-IN-1 can be used for the research of tumor-targeted autophagy inhibitors.

hsa-miR-320a-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.

hsa-miR-4708-5p 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.