Cancer Targeted Therapy

hsa-miR-5010-3p 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.

hsa-miR-6781-3p 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.

mmu-miR-1933-3p 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.

mmu-miR-6363 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-7228-5p 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.

Amino-PEG14-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.

PROTAC VEGFR-2 degrader-2 is a VEGFR-2 (KDR) PROTAC degrader with weak inhibitory activity against VEGFR-2 (IC₅₀ > 1 μM). It is applicable to the research of cancer-related pathological angiogenesis.

Boc-N-amido-PEG4-C3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC₅₀ of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC₅₀ values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.

hsa-miR-12130 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.

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.

HDAC6-IN-79 is a HDAC6 inhibitor with an IC₅₀ of 98.40 nM, and it also exhibits inhibitory activity against other HDAC subtypes (HDAC1: 639.0 nM, HDAC2: 798.9 nM, HDAC8: 865.7 nM, HDAC4: 1187 nM). HDAC6-IN-79 induces acetylation of α-tubulin and histone H3, reduces the viability of cancer cells, activates the autophagy pathway and induces apoptosis. HDAC6-IN-79 can be used for research related to urothelial carcinoma (bladder cancer).

DMG-PEG2000-A7R (DMG-PEG2000-Mal-Cys-ATWLPPR) is a functionalized PEGylated phospholipid conjugate composed of three modular components: dimyristoylglycerol (DMG) as a lipid anchoring group, a polyethylene glycol (PEG) spacer arm with a molecular weight of 2000 Da, and an A7R (HY-P1663) peptide as a terminal targeting/functional ligand. DMG-PEG2000-A7R can be used in research such as tumor angiogenesis-targeted drug delivery.

Hydroxymycotrienin B is an ansamycin group antibiotic (triene-ansamycin) found in culture broths of Bacillus sp. BMJ958-62F4. Hydroxymycotrienin B inhibits HPV-positive cervical cancer cell growth 3~10 times more strongly than HPV-negative cervical cancer cells. Hydroxymycotrienin B can be used for the research of human cervical cancer.

CES (CESPLLSEC) is a homing peptide targeting Synaptosomal associated protein 25 (SNAP25). CES specifically homes in intracranial U87MG and the WT-glioblastoma (GBM) model. CES can be used as a targeting peptide for drug delivery for cancers research.

SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC₅₀ of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice.

TX2-120-1 possesses the ability to bind to Her3, with an IC₅₀ value of 56 nM for Her3. TX2-120-1 can be used for the synthesis of TX2-121-1 (HY-118998).

Boc-Pyrrolidine-PEG2-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.