hnscc

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

Perindoprilat (Perindoprilate) is an angiotensin-converting enzyme inhibitor.

COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.

Monalizumab is a novel immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab is a humanized monoclonal antibody against NKG2A that induces IFN-γ production, thereby activating natural killer cell function. Monalizumab has antitumor activity and can be used to study neck squamous cell carcinoma (HNSCC).

(Rac)-AMXT-1501 4HCl is a polyamine transport inhibitor that inhibits polyamine transport and acts synergistically with cisplatin in HNSCC. (Rac)-AMXT-1501 4HCl has potential antimicrobial activity and inhibits neuroblastoma cell proliferation and pneumococcal pod biosynthesis by targeting ornithine decarboxylase and polyamine transport.

Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.

Pulrodemstat HCl is an orally active, selective and potent lysine demethylase-1 (LSD1) inhibitor, and a selective KDM1A inhibitor, with anticancer and anti-proliferative activities, inhibiting HNSCC cell proliferation and migration Inhibits the growth of head and neck squamous cell carcinoma by triggering apoptosis.

Pyrazofurin is a pyrimidine nucleoside analogue that potently inhibits cell proliferation and DNA synthesis by targeting UMP synthase, while also acting as a highly sensitive orotate-phosphoribosyltransferase inhibitor with IC50 values ranging from 0.06 to 0.37 μM in Hep-2, HNSCC-14B, and HNSCC-14C cell lines, supporting the use of Pyrazofurin as a mechanistic probe for nucleotide biosynthesis inhibition and antiproliferative research.

PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. This compound is applicable in anticancer research.

Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.

SVC112 is a translation elongation inhibitor that obstructs the periodic dissociation of EF2 from the ribosome, thereby inhibiting the elongation phase of translation. It demonstrates inhibitory activity in multiple cancer cell lines, including acute myeloid leukemia (AML), multiple myeloma, colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC). SVC112 preferentially impedes ribosomal processing of mRNA, reducing cancer stem cell (CSC)-related proteins such as Myc and Sox2. In hematological cancer cell lines, it induces apoptosis, whereas in colorectal cancer lines, the phosphorylation of c-Myc correlates with sensitivity to SVC112. The compound effectively inactivates HNSCC stem cells in vitro and prevents tumor regrowth in mouse HNSCC xenograft models. SVC112 is applicable for research on head and neck squamous cell carcinoma.

JH-XIV-68-3 is a selective inhibitor of the DYRK1A/B macrocycle, acting specifically on DYRK1A and DYRK1B in biochemical and cellular assays, and exhibiting antitumor effects in head and neck squamous cell carcinoma (HNSCC) cell lines.

JH-XVII-10 is a selective, orally active and potent inhibitor of DYRK1A (IC50: 3 nM) and DYRK1B (IC50: 5 nM).JH-XVII-10 exhibits antitumor effects in squamous cell carcinoma of the neck (HNSCC) cell lines.

GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment in the management of HNSCC.

NR2F1 agonist 1, a specific nuclear receptor NR2F1 activator, initiates dormancy programs in cancer cells by upregulating NR2F1 and its target genes controlling dormancy. This compound promotes neural crest-like features and suppresses growth in head and neck squamous cell carcinoma (HNSCC) through NR2F1 activation. Moreover, NR2F1 agonist 1 demonstrates tumor growth inhibition in a mouse primary tumor model.

Petosemtamab (MCLA 158) is a highly potent monoclonal antibody against EGFR (Kd: 0.22 nM) and LGR5 (Kd: 0.86 nM). Petosemtamab promotes EGFR signaling disruption and receptor breakdown in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

Izalontamab (SI-B001) is a bispecific EGFR/HER3 monoclonal antibody that binds to both EGFR×EGFR homodimers and EGFR×HER3 heterodimers, thereby blocking downstream pathways. It is applicable for locally advanced or metastatic epithelial tumours, such as non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC).

HN-1, a 12-mer peptide with specificity for head and neck squamous cell carcinoma (HNSCC), penetrates tumor tissue and facilitates the translocation of agents across cell membranes [1].

FOSL1 degrader 1 (4) is a potent T-5224-PROTAC that effectively degrades FOSL1 (AP-1), thereby suppressing the expression of cancer stemness genes in HNSCC. By degrading FOSL1, it inhibits tumor growth and effectively eliminates cancer stem cells in HNSCC tumors. This compound demonstrates an efficacy 30 to 100 times greater than that of T-5224.

Caroverine is a potential chemotherapeutical agent in HNSCC cell lines.

Eclutatug (ALE C04) is a humanised antibody targeting claudin-1 (CLDN1), which can be used for the treatment of tumours and organ fibrosis indications, such as head and neck squamous cell carcinoma (HNSCC).

Petosemtamab (FUT8-KO) is a variant of Petosemtamab with the fucosyltransferase 8 gene (FUT8) knocked out. Petosemtamab is a monoclonal antibody (mAb) targeting EGFR (with a Kd of 0.22 nM) and LGR5 (with a Kd of 0.86 nM). This antibody disrupts EGFR signaling and causes receptor degradation in LGR5+ cancer cells. It is applicable in research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

CHS-114 (SRF-114) is a fully human IgG1 antibody targeting the (CCR8) receptor. It shows potential for research in head and neck squamous cell carcinoma (HNSCC). The isotype control for CHS-114 can be referred to as HumanIgG1kappa, Isotype Control.

CDX-3379 is a humanized monoclonal antibody inhibitor that targets ErbB3. By binding to ErbB3, CDX-3379 prevents its dimerization with other receptors, thus inhibiting ErbB3 phosphorylation. This compound can also inhibit the growth and proliferation of tumor cells. CDX-3379 shows potential for research in tumors expressing ErbB3 and NRG1, such as those found in HNSCC.