Cancer Targeted Therapy

DMG-PEG2000-CGKRK (DMG-PEG2000-Mal-Cys-CGKRK) is a functionalized PEGylated phospholipid conjugate composed of three modular components: dimyristoylglycerol (DMG) as a lipid anchoring group, a 2000 Da polyethylene glycol (PEG) spacer arm, and a CGKRK peptide as a terminal targeting/functional ligand. DMG-PEG2000-CGKRK can be used in research on tumor angiogenesis-targeted drug delivery, among other applications.

ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1).

2’-Deoxy-N6-(4-methoxybenzyl)adenosine 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.

YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC₅₀ of 19.9 μM. YM-08 also is inhibitor of Hsp70.

rno-miR-298-3p 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.

dTBP-3 is a fully D-configured polypeptide competitive inhibitor that targets TIGIT. dTBP-3 can competitively occupy the binding interface between TIGIT and its ligand PVR, block TIGIT-mediated immunosuppressive signals, and reverse the immune exhaustion of NK cells and CD8⁺ T cells. dTBP-3 possesses anti-proteolytic activity and tumor tissue penetration ability, and can also enhance the tumor penetration capacity and cellular internalization efficiency of nanocarriers. dTBP-3 can be used in studies related to liver cancer, triple-negative breast cancer and non-small cell lung cancer.

Anti-5T4 scFv-Fc Antibody (ASN004 Antibody) is a human IgG1 monoclonal antibody targeting TPBG. Anti-5T4 scFv-Fc Antibody (ASN004 Antibody) can be used in cancer research. The recommended isotype control is human IgG1 kappa (HY-P99001).

hsa-miR-4284 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-5196-3p 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.

PROTAC BRAF-V600E degrader-2 is a PROTAC degrader targeting BRAF-V600E. The K_d values of PROTAC BRAF-V600E degrader-2 for BRAF and BRAF-V600E are 14.4 nM and 9 nM, respectively. PROTAC BRAF-V600E degrader-2 selectively degrades BRAF-V600E but does not degrade wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits the MEK/ERK kinase cascade and suppresses the growth of melanoma cells. PROTAC BRAF-V600E degrader-2 can be used in studies related to melanoma and colon cancer.

KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC₅₀ values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes.

HS-PEG5-CH2CH2N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. HS-PEG5-CH2CH2N3 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.

N-Ethyl-333-trifluoro-N-methylpropanamide-PEG2-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Pseudolycorine is an Amaryllidaceae alkaloid with anticancer activity.

Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [³H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC₅₀ values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells.

TMU454 is an ASGPR-targeting GalNAc-PROTAC BRD4 degrader conjugate. TMU454 undergoes ASGPR-mediated endocytosis and CTSB cleavage to release MZ1, which selectively degrades BRD4 in ASGPR-positive hepatocellular carcinoma cells via the VHL/UPS/proteasome pathway. TMU454 inhibits cancer cell proliferation and colony formation, and suppresses tumor growth in vivo. TMU454 can be used for research related to hepatocellular carcinoma.

mmu-miR-339-3p 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-6966-3p 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.

PD-1/PD-L1-IN-64 is a PD-1/PD-L1 interaction inhibitor. PD-1/PD-L1-IN-64 induces PD-L1 internalization and oligomerization, enhances T-cell activation, proliferation, and cancer cell elimination. PD-1/PD-L1-IN-64 can be used for the research of cancer.

AFG206 is a first-generation ATP competitive “type II” FLT3 inhibitor. AFG206 potently inhibits cell proliferation (IC₅₀ around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia.