thyroid cancer

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Rhodiolin, a natural product from Rhodiola rosea, blocks glycolysis of glucose 6-phosphate isomerase (GPI) in human papillary thyroid cancer (PTC), inhibits phosphorylation of the PI3K/AKT/mTOR signaling pathway and induces apoptosis of PTC cells.

Crolibulin (EPC2407) is an inhibitor of small molecule tubulin polymerization.

L-Thyroxine sodium salt pentahydrate (Sodium levothyroxine pentahydrate) is a thyroid hormone with anticholesterol activity that inhibits the release of thyroid hormones from thyroid cancer nodules and is used in immune and endocrine disorders such as hypothyroidism, myxedema, cretinism and obesity. diseases, such as hypothyroidism, myxedema, cretinism and obesity.

Vandetanib Fumarate is an orally available tyrosine kinase inhibitor. Vandetanib Fumarate works by blocking RET (REarranged during Transfection), vascular endothelial growth factor receptor (VEGFR-2, VEGFR-3), and epidermal growth factor receptor and to a

XMD15-44, a RET kinase inhibitor, demonstrates potent growth-inhibitory effects on RAT1 cells transformed by RET/C634R and RET/M918T, with IC50 values of 11.5 nM and 8.3 nM, respectively. It effectively inhibits RET kinase activity and signaling in human thyroid cancer cell lines harboring oncogenic RET alleles, thereby reducing cell proliferation.

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET/C634R and RET/M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.

GPX4-IN-13 (compound 16), a GPX4 inhibitor, exhibits anticancer properties by diminishing the expression of GPX4, thereby reducing thyroid cell proliferation and inducing ferroptosis. Additionally, this compound effectively inhibits the growth of three distinct thyroid cancer cell lines: N-thy-ori-3-1 (IC 50 =8.39 μM), MDA-T32 (IC 50 =10.28 μM), and MDA-T41 (IC 50 =8.18 μM).

NCATS-SM4420 (Compound A35) is an orally effective ligand for the thyroid-stimulating hormone receptor (TSHR) that inhibits the proliferation of MDA-T32 and MDA-T85 cells both in vitro and in vivo, with IC50 values of 0.71 μM and 0.38 μM, respectively. Additionally, it suppresses the metastasis of MDA-T85F1 in mice. NCATS-SM4420 holds potential for research in the field of thyroid cancer.

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1)/BRM/SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

FHND5071 (1H) is a selective inhibitor of RET (rearranged during transfection) tyrosine kinase. It shows potential for research applications in RET-driven cancers, such as thyroid and lung cancer.

TRK-IN-32 is a potent TRK inhibitor. It significantly suppresses TRKWT, TRKG595R, and TRKG667C with IC50 values of 0.08 nM, 2.14 nM, and 0.68 nM, respectively. Additionally, TRK-IN-32 exhibits antiproliferative activity against various Ba/F3 cell lines transformed by wild-type, xDFG mutant, solvent front, and gatekeeper mutant TRK fusion proteins. It also induces apoptosis in Ba/F3-TRKAWT and Ba/F3-TRKAG667C cells. TRK-IN-32 is applicable in research on various cancers, including thyroid cancer and secretory breast cancer.

AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numero

CMLD-2 is an inhibitor of HuR-ARE interaction (Ki: 350 nM) that competitively binds HuR protein and disrupts its interaction with adenine element-rich (ARE) mRNA targets.CMLD-2 induces apoptosis and exhibits antitumor effects through MAD2 downregulation. CMLD-2 (1-75 μM ; 24-72 h) had an inhibitory effect on the viability of thyroid cancer cells.CMLD-2 (20-30 μM ; 24-48 h) activated caspases and induced apoptosis in H1299 and A549 cells.CMLD-2 (30 μM ; 24-48 h) induced G1 cell cycle arrest in H1299 and A549 cells and mitochondrial perturbation. CMLD-2 (30 μM ; 24-48 h) reduced the expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells.CMLD-2 (35 μM ; 72 h) decreased the directional migration ability of SW1736, 8505C, BCPAP and K1 cells.CMLD-2 induced the migration of SW1736, 8505C, BCPAP and K1 cells with a strong decrease in MAD2 mRNA levels.

Monoethyl phthalate, a metabolite of diethyl phthalate, serves as a urinary biomarker for phthalate exposure and indicates potential risks of thyroid cancer and benign nodules.

RET-IN-9 is a potent inhibitor of RET, a single-channel transmembrane receptor tyrosine kinase involved in kidney and enteric nervous system development, as well as in maintaining homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 is potentially useful in studying RET-related diseases, including non-small cell lung cancer and medullary thyroid cancer.

CUDC-907 mesylate is a small molecule inhibitor of histone deacetylase and PI3 kinase developed by Curis. It is investigated in clinical trials for the treatment of relapsed or refractory lymphomas, thyroid cancer, multiple myeloma, breast cancer and other malignancies.

GNE-8625 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.

EGCG-4″-sulfate, a predominant polyphenol in green tea, demonstrates notable anticancer, antioxidant, and anti-inflammatory effects, particularly against colorectal cancer, myeloid leukemia, and thyroid carcinoma [1] [2] [3] [4]. This compound not only inhibits cell proliferation and triggers cell apoptosis but also suppresses the activity of glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2), highlighting its important role in cancer prevention and treatment.

Spartalizumab (PDR001) is a humanized immunoglobulin G4 monoclonal antibody that selectively binds to PD-1 at low concentrations, exhibiting high activity. It blocks the interaction with PD-L1 and PD-L2, making it suitable for studying undifferentiated thyroid cancer (ATC).

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

Niacinamide ascorbate is a vitamin complex that combines niacinamide (vitamin B3) and ascorbic acid (vitamin C). This compound is known to reduce the risks associated with exposure to ionizing radiation, including radiation-induced acute leukemia, breast cancer, thyroid cancer, and other somatic and genetic mutations.

8-Azaadenosine, a powerful ADAR1 (ADAR1) and A-to-I editing inhibitor, effectively blocks RNA editing and suppresses proliferation, 3D growth, invasion, and migration in thyroid cancer cells.

Labetuzumab is a humanized anti-carcinoembryonic antigen (CEA) monoclonal antibody with anticancer activity that inhibits tumor growth and is used in the study of thyroid and colorectal cancer (CRC).