ca 1

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.

CA inhibitor 1 (GS-6207 analog) is a potent inhibitor of the HIV capsid.

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

CAⅡ-IN-1 (compound 2i) is an inhibitor of the CA Ⅱ isozyme, exhibiting an IC50 of 0.44 µM. This compound is utilized in metabolic research.

AChE/CA I-IN-1 (Compound 2g) acts as an inhibitor for both AChE and hCA I, with Ki values of 1.85 µM and 0.53 µM, respectively. It has shown potential applications in the research of Alzheimer's disease, glaucoma, and epilepsy.

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 IX-IN-1 (compound 12g) is a potent and highly selective hCA IX inhibitor (IC50: 7 nM) with demonstrated antitumour effects.

ICA 110381 is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

Eldacimibe (WAY-ACA-147) is an ACAT2 inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, study of atherosclerosis and hypercholesterolemia.

GAL-021 an intravenous BKCa-channel blocker.

Probucol (DH-581), an anti-hyperlipidemic drug, can lower the level of cholesterol in the bloodstream by increasing the LDL catabolic rate.

Adenosine (D-Adenosine) is a natural product, a ribonucleoside consisting of adenine bound to ribose. Adenosine has vasodilatory, antiarrhythmic and analgesic effects.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

Rucaparib (PF-01367338) is a PARP protein inhibitor (PARP-1 Ki=1.4 nM) and hexose hexose-6-phosphate dehydrogenase (H6PD) inhibitor with oral activity. Rucaparib exhibits antitumor activity, with activity against desmoplasia-resistant prostate cancer (CRPC).

(E)-β-Farnesene (trans-β-Farnesene) is a sesquiterpene hydrocarbon found in Phlomis aurea Decne, serving as the primary component of many aphid alarm pheromones that disrupt feeding. It also impairs the development and survival of Chilo suppressalis larvae by disrupting their hormone balance.

PD-1-IN-1 is a programmed cell dealth-1inhibitor. PD-1-IN-1 can be used as an immune modulator.

BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 with an IC50 of 0.53 μM and a Ki of 0.71 μM.

BRCA1-IN-2 is a cell membrane-crossing BRCA1 protein-protein interaction (PPI) inhibitor with antitumor activity that acts by disrupting the interaction of BRCA1 (BRCT)2 with proteins.

ICA-105665 (PF-04895162) is a potent and orally active opener of neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects [1][2][3][4].