ca²⁺

Sortase A, S. aureus (non-Ca2+-dependent), is a transpeptidase found in numerous Gram-positive bacteria, crucial for the recruitment of surface proteins. It plays a significant role in linking various molecules on the cell surface.

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a selective inhibitor of Cathepsin B (IC50=36.3 nM). CA-074 methyl ester has neuroprotective, anti-inflammatory and anti-cancer effects.

Calcium trinatrium diethylenetriaminepentaacetic acid hydrate (Ca-DTPA trisodium salt hydrate) is a metal chelator and a nontoxic inhibitor of CMV replication, as well as a useful antidote in cases of acute cadmium intoxication.

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.

CA-170 is an orally bioavailable dual inhibitor of VISTA and PD-L1 that selectively restores T-cell proliferation and effector function suppressed by immune checkpoint signaling, while demonstrating minimal off-target activity across a broad receptor and enzyme panel, making CA-170 a valuable compound for immuno-oncology research and immune checkpoint modulation studies.

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.

CAIX-IN-3 (Compound 27) is a selective and potent inhibitor of carbonic anhydrase IX (CAIX), with an IC50 of 0.48 nM.

CAIX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

CAIX/VEGFR-2-IN-2 (compound 5e) is a dual-target inhibitor with potent inhibitory effects on CAIX (KI=3.1 μM) and VEGFR-2 (IC50=32.1 nM). This compound is applicable in research involving pancreatic cancer (PANC1), breast cancer (MCF7), and prostate cancer cells (PC3).

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-II/TNAP-IN-1 is a novel 1,3-disubstituted thiourea derivative that acts as a dual inhibitor of carbonic anhydrase II (CA-II) and tissue-nonspecific alkaline phosphatase (TNAP). The compound is an essential tool for investigating cancer metabolism and enzyme-mediated tumor microenvironment regulation, aiming to enhance anti-tumor efficacy by jointly inhibiting key enzymes involved in pH regulation and mineralization.

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.

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

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor that works by inhibiting autophagosome-lysosome fusion.

IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.

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

Compound 4H is a potent carbonic anhydrase inhibitor with an IC50 value of 0.033 μM [1].

Ir-CA is an antitumor agent that accumulates in mitochondria, inducing mitochondrial dysfunction, apoptosis, and autophagy. It initiates mitophagy and cell cycle arrest to kill Cisplatin-resistant A549R cells and effectively inhibits metastasis by inhibiting MMP-2/MMP-9 [1].

CAIX-IN-2 (Compound 9o) is an inhibitor of carbonic anhydrase (CA), targeting CAIX, CA XII, and CAII with IC50 values of 5.6, 7.4, and 430 nM, respectively. This compound effectively inhibits the proliferation of cancer cells such as HCT-116, SW480, MDA-MB 231, and MCF-7, with IC50 values ranging from 14.63 to 29.33 µM. CAIX-IN-2 also integrates into DNA, causing cell cycle arrest at the G1/S phase and inducing apoptosis in MDA-MB-231 cells. Furthermore, it disrupts mitochondrial membrane potential (MMP), elevates intracellular ROS levels, leading to mitochondrial damage, and inhibits the migration of MDA-MB-231 cells. In mouse models, CAIX-IN-2 has demonstrated antitumor activity.

CA77.1(CA) is a novel chaperon-mediated autophagy (CMA) activator for the treatment of Alzheimer's disease (AD).

CA-CoA (CA-Coenzyme A) is a derivative of coenzyme A.

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.