hcc

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Silymarin (Silybin B) (Silybin B) is a polyphenolic flavonoid that extracts from the milk thistle or seeds of Silybum marianum. It is used in the prevention and treatment of liver diseases.

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1 3 compared to other inhibitors.

GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).

Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

(E)-PHCCC, acting as a positive allosteric modulator (PAM) of the mGluR4, enhances the activity of the receptor's endogenous ligand (glutamate). It demonstrates activity in a calcium mobilization assay in CHO cells, with an EC50 of 3.2 μM.

THCCC, a PHCCC analog, is a dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulator.

PHCCC ((-) PHCCC) is a Group I metabotropic glutamate receptor antagonist and a positive allosteric modulator of mGluR4. It also is a potent to antagonism for mGluR2 and mGluR8.

(1R,3S)-THCCA-Asn (4j) is a selective inhibitor of thrombin with an IC50 range of 0.07-0.14 μM and exhibits anti-thrombotic effects.

Scutellarin (Scutellarein-7-glucuronide), an active flavone isolated from Scutellaria baicalensis, can inhibit RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts, and down-regulate the STAT3 Girdin Akt signaling in HCC cells.

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

XST-14 is a competitive and specific inhibitor of ULK1 (IC50: 26.6 nM).XST-14 blocks autophagy by inhibiting the phosphorylation of ULK1 downstream substrates.XST-14 induces apoptosis and inhibits the growth of HCC cells.

Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Triglycidyl isocyanurate (Teroxirone) is a triazene triepoxide with antineoplastic and antiangiogenic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. It induces cell apoptosis and can be used for cancer research[1][2]. Triglycidyl isocyanurate is also used in various polyester powder coatings in the metal finishing industry.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid and a ligand for vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1), exhibiting neuroprotective activity, inhibiting spasm, and enhancing cisplatin chemotherapy sensitivity by inducing ferroptosis in HCC cells in vivo. It induces ferroptosis in liver cancer cells via binding to MICU1.

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.