Cancer Targeted Therapy

mmu-miR-6929-5p 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-99a-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.

KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC₅₀ = 123 nM) and human HO-1: IC₅₀ = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1⁺ perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer.

Grp94-IN-3 (Compound 47) is a selective ATP competitive inhibitor of Grp94, with a K_d value of 76 nM. Grp94-IN-3 has a much lower affinity for Hsp90α, with a K_d value of 9.17 μM. Grp94-IN-3 induces the degradation of integrin α2 (Integrin α2) in MDA-MB-231 cells and reduces the intracellular accumulation of mutant cardiac proteins in human trabecular meshwork cells. Grp94-IN-3 can be used for the study of metastatic cancer and open-angle glaucoma.

Anti-Rat CD80/B7-1 Antibody (3H5) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to rat CD80/B7-1. Anti-Rat CD80/B7-1 Antibody (3H5) blocks a costimulatory signals for T-cell activation. Anti-Rat CD80/B7-1 Antibody (3H5) can be used for the researches of cancer and immunology.

Axl ligand-1 is a highly selective ligand for AXL kinase, exhibiting higher selectivity for AXL over 72 human kinases. Axl ligand-1 serves as a Ligand for Target Protein for PROTAC, which is applied to develop PROTAC degraders with anti-tumor activity, such as PROTAC Axl Degrader 1 (HY-144624). Axl ligand-1 is applicable to breast cancer-related research.

hsa-miR-3120-5p 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.

IDO1-IN-17 (I-4) is an IDO1 inhibitor, with an IC₅₀ of 0.44 μM in hela cells.

ANO1-IN-3 (Compound 3n) is a potent and selective ANO1 inhibitor with an IC₅₀ of 1.23 μM. ANO1-IN-3 induces apoptosis.

hCAIX-IN-15 is a potent hCA IX inhibitor with a K_i value of 38.8 nM. hCAIX-IN-15 shows good broad-spectrum anticancer activity and can be used for cancer research.

2’,3’,5’-Tri-O-benzoyl-4-thiouridine 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.

E3 ligase Ligand-Linker Conjugate 29 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. E3 ligase Ligand-Linker Conjugate 29 can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

Pyrene-PEG5-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC SMARCA2/4 degrader-25 is a selective SMARCA2/SMARCA4 PROTAC degrader with selective anti-tumor activity. PROTAC SMARCA2/4 degrader-25 is activated by endogenous GSH, forms a ternary complex with SMARCA2 or SMARCA4 and VHL E3 ubiquitin ligase, and mediates degradation via the proteasome pathway. PROTAC SMARCA2/4 degrader-25 induces DNA damage and apoptosis, and inhibits cancer cell proliferation. PROTAC SMARCA2/4 degrader-25 is applicable to lung cancer-related research.

SJ46411 is a potent ligand for KLHDC2, with a K_d of ~260 nM measured by isothermal titration calorimetry (SPR K_d = 0.5 μM, TR-FRET IC₅₀ = 3.9 μM, ΔTm = 6.0 °C).

APN- NH2 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. APN- NH2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

LB42908 is a potent, selective and orally active farnesyltransferase inhibitor. LB42908 inhibits farnesylation of H-Ras, K-Ras with IC₅₀ values of 0.9 nM, 2.4 nM for H-Ras, K-Ras, respectively. LB42908 shows antiproliferative activity. LB42908 shows antitumor activity.

ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19.

Propargyl-PEG9-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG9-THP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

hsa-miR-4761-5p 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.