Cancer Targeted Therapy

MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice..

AM-Imidazole-PA-Boc is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966).

TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC₅₀ of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC₅₀ of 3.5 μM.

PRMT5-IN-37 (compound 29) is an orally active PRMT5 inhibitor and can be used for study of cancer.

hsa-miR-150-5p 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.

CK2-IN-10 (31), an allosteric CK2 inhibitor, can be used in the research of cancer.

DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype.

G-631 is an orally active tankyrase(TNKS1/TNKS2) inhibitor. G-631 stabilizes AXIN and inhibits the Wnt/β-catenin signaling pathway. G-631 can be used in studies related to cancers such as colorectal cancer.

Alphitolic acid (Aophitolic acid) is an anti-inflammatory triterpene could found in quercus aliena. Alphitolic acid blocks Akt–NF-κB signaling to induce apoptosis. Alphitolic acid induces autophagy. Alphitolic acid has anti-inflammatory activity and down-regulates the NO and TNF-α production. Alphitolic acid can be used for cancer and inflammation research.

Azidoethyl-SS-ethylamine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azidoethyl-SS-ethylamine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Fmoc-Hyp(Bom)-OH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Hyp(Bom)-OH is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs<

hsa-miR-629-5p 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.

CDDO-biotin is an IKKβ inhibitor with cancer cell inhibitory activity. CDDO-biotin directly interacts with and oxidizes Cys-179 in the activation loop of IKKβ, forming an adduct with wild-type IKKβ. CDDO-biotin can be used in the research of myeloid leukemia, osteosarcoma, multiple myeloma, lung cancer, breast cancer and pancreatic cancer.

MS33 is a potent WDR5 degrader, with K_ds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.

Azido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG10-acid is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Methyltetrazine-PEG4-SS-NHS ester is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Methyltetrazine-PEG4-SS-NHS ester is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

PIN1 ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PIN1 ligand-1 can be used for synthesis PROTAC PIN1 degrader-1 (HY-168037).

NH2-MPAA-NODA TFA is a nitroveratryl-based photocleavable linker, it has a NODA motif and a methyl phenyl acetic acid (MPAA) backbone. NH2-MPAA-NODA can be used as a radiolabel by labeling with ¹⁸F-fluoride.

BJG-05-039 is an inhibitor targeting PAK1, with an IC₅₀ of 233 nM against human PAK1. BJG-05-039 induces the selective degradation of PAK1 and inhibits its kinase activity by conjugating NVS-PAK1-1 (HY-100519) with Lenalidomide (HY-A0003) to recruit Cereblon. BJG-05-039 can be used in research related to breast cancer and ovarian cancer.

BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC₅₀ towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC₅₀ between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules.