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.

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

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.

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.

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 is a natural polyphenolic flavonolignan mixture extracted from the seeds of Silybum marianum. It can inhibit tumor cell proliferation and angiogenesis, and improve insulin resistance, thus being widely used in liver disease-related research and adjuvant applications. Studies have shown that silymarin exhibits inhibitory activity against the SARS-CoV-2 main protease, and it has potential research value in the mechanism-related studies of COVID-19.

Nizatidine (Acinon) is a competitive and reversible histamine H2-receptor antagonist with antacid activity.

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.

PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].

Glumetinib (SCC244) is a novel potent and selective inhibitor of c-Met kinase (IC50: 0.42 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.

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) is a potent STAT3 inhibitor that reduces the ability of STAT3 to bind to DNA and also has a good growth inhibition effect on liver cancer cells [1].

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

Avicularin (Fenicularin) has anti-allergic, anti-inflammatory, hepatoprotective, antioxidant, anti-tumor and other activities. It ameliorates human hepatocellular carcinoma by modulating the activities of NF-κB(p65), COX-2, and PPAR-γ. In LPS-stimulated RAW 264.7 macrophages, it exerts anti-inflammatory activity by inhibiting the ERK signaling pathway.

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

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

(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.