Cancer Targeted Therapy

Tigecycline (Standard) is the analytical standard of Tigecycline. This product is intended for research and analytical applications. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC₅₀ and MIC₉₀ are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.

Ac-WEHD-AFC is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation.

VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor.

PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis.

EGFR/HER2-IN-15, a dihydropyrimidine, is a potent EGFR/HER2 inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR^wt activity with an IC₅₀ of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects.

VEGF-IN-1 (compound 6) can reduce the release of VEGF in U87-MG cells and inhibit angiogenesis in vitro. VEGF-IN-1 can inhibit cell proliferation by inducing autophagy in tumor cells, with an IC₅₀ value of 28.35 μM for U87-MG cells.

DSPE-PEG5000-F3 is a PEG compound which composed of DSPE and a nucleolin targeting peptide (F3). F3 peptide can specifically bind to cell surface nucleolin and undergo an effective cell surface to nucleus transport. DSPE-PEG5000-F3 can be used for drug delivery.

hsa-miR-3153 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-4664-3p 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.

hsa-miR-6070 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-8072 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-3547-5p 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-6989-5p 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.

rno-miR-29b-1-5p 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.

RIPK2-IN-3 (FCG806791773) is a RIPK2 inhibitor. RIPK2-IN-3 inhibits recombinant truncated RIPK2 with an IC₅₀ of 6.39 μM. RIPK2-IN-3 can be used for research of inflammation and cancer.

N,N-Diethanol amine-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

NH2-PEG-phenol-PEG-COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC BRD4 Degrader-14 (HY-138637).

COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC₅₀ of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.

Anticancer agent 344 is a heterobifunctional anticancer compound with moderate cancer cell growth inhibitory activity, and it also exhibits inhibitory activity against ERα-overexpressing cells. Anticancer agent 344 can be used in cancer-related research.

c-Fms-IN-14 (Example 76) is a c-Fms inhibitor with an IC₅₀ value of 4 nM. c-Fms-IN-14 can be used for research of cancer and autoimmune diseases.