Cancer Targeted Therapy

Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.

hsa-miR-8081 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-3620-3p 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.

mmu-miR-6994-3p 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.

rno-miR-3084a-1-5p 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.

Losmapimod (GSK-AHAB; GW856553X) hydrochloride is an orally active p38α/β MAPK inhibitor, with pK_i values of 8.1 and 7.6 for p38α and p38β, respectively. Losmapimod hydrochloride reduces DUX4 expression, thus exerting efficacy in facioscapulohumeral muscular dystrophy. By inhibiting MAPK/NF-κB, Losmapimod hydrochloride reduces apoptosis of epileptiform hippocampal neurons, and exhibits anti-allodynia and anti-hyperalgesic activities. Losmapimod hydrochloride blocks the entry and fusion of Lassa fever virus (LASV). Losmapimod hydrochloride overcomes tyrosine kinase inhibitor resistance in non-small cell lung cancer (NSCLC). Losmapimod hydrochloride inhibits myocardial senescence and inflammation, and possesses cardioprotective activity against cardiotoxicity.

TGFβRI-IN-6 (compound 22) is a potent TGFβRI inhibitor with an IC₅₀ value of 0.55 nM. TGFβRI-IN-6 has the potential to enhance anti-tumor immunity.

Trimidox (VF-233) is a ribonucleotide reductase inhibitor with antileukemic activities. Trimidox inhibits the growth of human promyelocytic leukemia HL-60 cells with an IC₅₀ of 35 μM.

CH2COOH-PEG12-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

hsa-miR-302e 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-4521 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-5685 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.

AR ligand-37 is a PROTAC target protein ligand that can be used to synthesize BMS-986365 (HY-158101).

Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC₅₀ for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460.

HSN608 is an orally active, potent RET G810 mutant inhibitor. HSN608 inhibits G810C, G810R, G810D. HSN608 induces Apoptosis. HSN608 inhibits the Selpercatinib (HY-114370)-resistant RET(G810C) CDX tumors.

PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma.

TACC3-IN-5 (Compound 35) is a TACC3 inhibitor. TACC3 is a scaffold protein that is highly expressed in various tumors and regulates microtubule/centrosome stability via phosphorylation by Aurora A. TACC3-IN-5 inhibits the proliferation of triple-negative breast cancer cells. TACC3-IN-5 is applicable for triple-negative breast cancer research.

EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC₅₀ values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity.

FPR1 antagonist 2 (compound 25b) is a formyl peptide receptor 1 (FPR1) antagonist with an IC₅₀ of 70 nM. FPR1 antagonist 2 inhibits cell growth through a combined effect on cell proliferation and apoptosis and reduces cell migration, while inducing an increase in angiogenesis.

QI-18 is a fibroblast activation protein (FAP) inhibitor with the IC₅₀ of 0.50 nM, which is a 6.5-fold increase in potency over that of UAMC-1110 (HY-100684，IC₅₀ of 3.25 nM). QI-18 can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and study of tumors.