ca-i

Carboxyamidotriazole Orotate (L-651582 Orotate) is a cytostatic inhibitor of non-voltage-operated calcium channels and associated signaling pathways. As the orotate salt form of Carboxyamidotriazole (CAI), it is an orally bioavailable signal transduction inhibitor with in vitro antileukaemic activity, exhibiting anti-tumor, anti-inflammatory, and antiangiogenic effects.

Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It shows anti-inflammatory, anti-tumor, and antiangiogenic effects.

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

hCA-I/hCA-II-IN-1 (Compound P4) is a potent dual inhibitor of human carbonic anhydrase I (hCA-I) and human carbonic anhydrase II (hCA-II), with Ki values of 0.22 μM and 0.33 μM respectively. hCA-I/hCA-II-IN-1 is useful for research into diseases related to CA enzymes, including glaucoma, hypertension, and ulcers.

hCA-IN-1 (Compound 5u) is an hCA inhibitor with Ki values of 159.2 nM for hCA I, 4.8 nM for hCA II, 15.5 nM for CAIX, and 2 nM for CAXII. It demonstrates broad-spectrum anticancer activity against melanoma, breast cancer, and colon cancer cells. ADME predictions indicate that hCA-IN-1 has good solubility and oral bioavailability. This compound is useful in tumor research.

EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor of epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX), with IC50 values of 5.92 nM and 63 nM, respectively. This compound exhibits significant cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM. Additionally, EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, increases the BAX/Bcl-2 ratio, activates caspases, and causes cell cycle arrest at the G1 phase. It shows potential for breast cancer research.

CA-II/Dkk1-IN-1 (Compound 5d) is a dual inhibitor of CA-II and Dkk1, with an IC50 of 6.90 nM for CA-II. It exhibits significant antioxidant activity and exceptional DNA binding capability. CA-II/Dkk1-IN-1 is applicable in cancer research, including esophageal cancer, renal cancer, and lung cancer.

CA-IN-5g is an effective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase is isolated from Trypanosoma cruzi (TcCA).

Droxicainide is an antiarrhythmic agent, [used] to treat irregular heartbeats.

3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells.

Ketocaine(Rec 7-0518) is a local anesthetic commonly used in animal experiments with potential antitumor activity for pain relief.

Quinacainol (RP 54272) is a new antiarrhythmic compound with class I antiarrhythmic effects in rats.

Transcainide(R 54718), a new lidocaine analog, is an orally active antiarrhythmic agent.Transcainide blocks the open state of BTX-activated sodium channels in bovine heart and rat skeletal muscle.

Declopramide (OXI-104) is a novel chemosensitizer with antitumor activity that induces apoptosis and can be used to study colorectal cancer and inflammatory bowel disease.

Etidocaine is an amino acidamide that acts as a local anesthetic with fast onset and long-acting properties.

Indecainide (Ricainid) is a novel antiarrhythmic compound that is carcinogenic and can be used to study chronic stable ventricular arrhythmias secondary to coronary artery disease or cardiomyopathy.

Vadocaine (Vadocaina) is a novel analgesic compound for local anaesthesia and can be used to study the central nervous system and cardiovascular system.

Recainam is a novel, orally available compound with potent class I antiarrhythmic activity.

solpecainol is a sodium channel blocker used in the study of neurological and cardiovascular diseases.

Trapencaine is a newly synthesized carbamate type local anesthetic that induces conformational changes in sodium channels on hypertrophic cell membranes.

Pincainide is a novel beta-aminoaniline that inhibits, in a dose-dependent manner, diseases caused by abnormal norepinephrine vascular smooth muscle function.

Pilsicainide HCl (SUN 1165) is a pure sodium channel blocker

Methazolamide (CL 8490) is a carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.

Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor.