Cyclophilin Inhibitor

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Cyclosporin A (Standard) (Cyclosporine A (Standard)) is the analytical standard of Cyclosporin A (HY-B0579). This product is intended for research and analytical applications. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

RN-0001 is an inhibitor of Calcineurin and cyclophilin (Cyp), with K_i values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC₅₀ of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease.

Cyclosporin A-d₄ (Cyclosporine A-d₄) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.

Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a K_d of 5 nM, shows effective anti-HCV activity, with an EC₅₀ of 98 nM for HCV 2a.

C105SR is a cyclophilin D (CypD) inhibitor targeting to peptidyl-prolylcis-trans isomerase (PPIase). C105SR inhibits mitochondrial permeability transition opening (mPTP) with an IC ₅₀ of 5 nM. C105SR inhibits hypoxia and reoxygenation inudced hepatocyte apoptosis and increases the level of calcium retention capacity (CRC). C105SR exhibits hepaprotective effect in ischaemia-reperfusion injury (IRI) mouse model.

HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis.

CypA ligand-2 is the target protein ligand of PROTAC RJS308 (HY-173011). RJS308 is a PROTAC targeting CypA and exhibits antiviral activity.

Cyclosporin A-¹³C₂,d₄ (Cyclosporine A-¹³C₂,d₄) is the deuterated, ¹³C-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Cyclosporin A acetate-d₄ (Cyclosporine A acetate-d₄) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

Cyclosporin A-d₁₂ (Cyclosporine A-d₁₂) is the deuterated-labeled Cyclosporin A (HY-B0579). Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM. Cyclosporin A is a molecular glue, binds to cyclophilin and calcineurin, leading to inactivation of nuclear Factor of activated T Cells (NFAT) and a subsequent decrease in the immune response. Cyclosporin A also inhibits CD11a/CD18 adhesion.

CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC₅₀ value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.

CypD-IN-7 is a potent cyclophilin D (CypD/PPIF) inhibitor that inhibits CypD PPIase activity (Kⁱ = 2.4 nM) and provides protection against mitochondrial permeability transition pore (MPTP) opening. CypD-IN-7 can be used for pancreatitis research.

CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC₅₀ value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.

CypE-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypE-IN-1 has CypE affinity with IC₅₀ and K_i values of 0.013 μM and 0.072 μM, respectively. CypE-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.

CypD-IN-6 is a potent cyclophilin D (CypD/PPIF) inhibitor that inhibits CypD PPIase activity (Ki = 32 nM) and binds to CypD (Kd = 60 nM). CypD-IN-6 can be used for mitochondrial permeability transition pore (MPTP) related disease research such as ischemia-reperfusion injury and acute pancreatitis¹.

CypB-IN-1 (Compound 11) is an inhibitor of cyclophilin B (cyclophilin B) with a K_d value of 12 nM. CypB-IN-1 can be applied to the research field of metabolic dysfunction-associated steatohepatitis (MASH) and the liver fibrosis diseases resulting from it.

Cyclophilin inhibitor 3 (compound 7c) is a potent cyclophilin A (CypA) inhibitor with an potent anti-HCV activity (EC₅₀ of 4.2 μM).

CypD-IN-29 (compound 29) is an inhibitor of the Alzheimer's disease target CypD (KD=88.2 nM). CypD is a mitochondrial-specific cyclophilin that can bind to β-amyloid protein in brain mitochondria and promote the formation of mitochondrial permeability transition pore (mPTP).