Cancer Targeted Therapy

HSD1590 is potent ROCK inhibitor, with IC₅₀s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (K_ds<2 nM). HSD1590 displays low cytotoxicity.

hsa-miR-103a-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.

Fmoc-PEG5-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

BC-1258，an F-box/LRR-repeat protein 2 (FBXL2) activator，can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells，and profoundly inhibits tumor formation in mice.

HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with K_i values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects.

AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

Gedatolisib-d₈ (PKI-587-d₈) 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.

LYP-8 is an intracellular nicotinamide phosphoribosyltransferase (iNAMPT) PROTAC degrader with an IC₅₀ of 0.76 μM. LYP-8 recruits VHL E3 ligase to induce iNAMPT polyubiquitination and proteasome-dependent degradation, and inhibits iNAMPT enzymatic activity. LYP-8 reduces eNAMPT levels by degrading iNAMPT to decrease eNAMPT secretion. LYP-8 reduces intracellular NAD⁺ levels in cancer cells and proinflammatory cytokine levels (IL-6, TNF-α) in tumor tissue and serum. LYP-8 can be used for the research of colon cancer.

BCL-xL ligand 6 is a ligand for Bcl-xL that can be used in the synthesis of PROTACs.

hsa-miR-190a-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.

αvβ6-BP TFA is a selective αvβ6 binding peptide, and can be used for research of molecular imaging.

MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is a drug-linker conjugate for ADC, formed by conjugation of 7ethanol-10NH2-11F-Camptothecin (HY-156517) with the protease-cleavable MC-GGFG linker. MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is applicable for cancer research.

Boc-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC, which is composed of a linker Boc-Val-Cit-PAB (HY141141) and a Microtubule inhibitor MMAE (HY-15162). Boc-Val-Cit-PAB-MMAE can be used for ADC synthesis.

Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.

PPM-3 is a highly selective ERK5 PROTAC degrader that mediates the degradation of ERK5 protein by recruiting VHL. PPM-3 inhibits ERK5 kinase activity with an IC₅₀ of 62.4 nM. PPM-3-mediated ERK5 degradation exhibits a hook effect. PPM-3 exerts no significant direct inhibitory effect on the proliferation and migration of cancer cells. PPM-3 can be used in studies related to macrophage polarization and tumor immunity.

hsa-miR-30b-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.

Thalidomide-O-amido-C6-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

hsa-miR-195-3p 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.

Z56-L23 is a conjugate of RAS-targeting ADC cytotoxic payload-linker with anti-tumor activity. Z56-L23 can be conjugated with HER3 antibody, EGFR antibody or EGFRxHER3 bispecific antibody to form intact antibody-drug conjugates (ADCs). ADC molecules related to Z56-L23 effectively inhibit the proliferation of tumor cells and also significantly suppress tumor growth in xenograft mouse models. Z56-L23 can be used in the research of pancreatic cancer.

Filgotinib-d₄ is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.