Cancer Targeted Therapy

FmocNH-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan (HY-147057). DOTAGA-FAP-2286-ALB is a selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ value of 67.5 nM. DOTAGA-FAP-2286-ALB enhances tumor retention via albumin interaction, prolonging blood circulation and improving radiometal complex stability (e.g., with 111In and 225Ac). DOTAGA-FAP-2286-ALB is promising for research of radionuclide therapy (TRT) of FAP-positive solid tumors.

SCP1-IN-1 is a Small CTD Phosphatase 1 (SCP1) inhibitor with a human IC₅₀ of 10 μM. SCP1-IN-1 inactivates SCP1, promotes REST transcription factor degradation, and reduces REST transcriptional activity. SCP1-IN-1 can be used for the research of glioblastoma multiforme.

Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells.

Mal-amido-PEG24-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC₅₀s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition.

GCPII-IN-1 (Compound 2) TFA is a GCPII (also known as PSMA) inhibitor with a K_i of 44.3 nM. GCPII-IN-1 TFA can be used in the research of prostate cancer.

WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647).

DBCO-PEG4-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG4-PFP ester is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

Celecoxib-d₃ is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC₅₀ of 40 nM.

hsa-miR-424-5p 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.

5-AIQ (5-Aminoisoquinolin-1-one) is a PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.

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.

hsa-miR-223-3p 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.

TFAP4/Wnt/β-catenin-IN-1 (Compound A61) is an orally active TFAP4/Wnt/β-catenin inhibitor. TFAP4/Wnt/β-catenin-IN-1 has significant anticancer activity against a variety of cancer cells (such as gastric cancer, lung cancer, breast cancer, etc.), and has the strongest anticancer activity against MGC-803 gastric cancer cells (IC₅₀: 3.92 μM). TFAP4/Wnt/β-catenin-IN-1 induces apoptosis and cell cycle arrest (S phase) in cancer cells by inhibiting the TFAP4/Wnt/β-catenin signaling pathway. TFAP4/Wnt/β-catenin-IN-1 can be used in the study of gastric cancer.

NAE-IN-1 (compound X-10) is a potent NAE1 inhibitor. NAE-IN-1 induces apoptosis and cell cycle arrest at the G2/M phase. NAE-IN-1 increases ROS levels and prevents cell migration. NAE-IN-1 shows anti-proliferation activity.

Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.

(rac)-BDM88951 is the racemate of BDM88951 (HY-176778). BDM88951 (Compound 4 d) is a selective ERAP2 inhibitor with an IC₅₀ of 19 nM. BDM88951 significantly inhibits antigen presentation in HEK cells. BDM88951 can be used for research on autoimmune diseases and cancer.

3,4-Dibromo-Mal-PEG2-N-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.