2. Signaling Pathways
  3. Immunology/Inflammation
  4. Cyclophilin

Cyclophilin

Cyclophilins are enzymes that accelerate the rotation of the peptide bond in front of a proline residue. Cyclophilins are involved in a wide variety of cellular processes such as folding, posttranslational modifications and transport of proteins, assembly of essential cellular protein complexes, and cell signaling. Cyclophilins have been identified in a range of organisms, including mammals, plants, insects, fungi, and bacteria.

The prototypic cyclophilin A (CypA) is the most abundant member of the cyclophilin family in human tissue and the major player in the cellular PPIase activity. CypA as a host cell protein interacts with viral proteins and can thus promote or inhibit viral replication and infection of a variety of RNA viruses, most prominently HIV‐1 and HCV.

Cyclophilin Isoform Specific Products:

Cyclophilin Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0579
    Cyclosporin A
    		Inhibitor 99.94%
    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 also inhibits CD11a/CD18 adhesion.
    Cyclosporin A
  • HY-P0025
    NIM811
    		99.87%
    NIM811 ((Melle-4)cyclosporin; SDZ NIM811) is an orally bioavailable mitochondrial permeability transition and cyclophilin dual inhibitor, which exhibits potent in vitro activity against hepatitis C virus (HCV) .
    NIM811
  • HY-12559
    Alisporivir
    		99.03%
    Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.
    Alisporivir
  • HY-100731
    Cyclosporin
    		99.31%
    Cyclosporin is a cyclic decapeptide that could be isolated form the soil fungi Tolypocladium inflatum. Cyclosporin is an immunosuppressant thought to bind to cyclophilin in T-lymphocytes.
    Cyclosporin
  • HY-B0579R
    Cyclosporin A (Standard)
    		Inhibitor
    Cyclosporin A (Standard) is the analytical standard of Cyclosporin A. 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 also inhibits CD11a/CD18 adhesion.
    Cyclosporin A (Standard)
  • HY-173011A
    RJS308 TFA
    		Degrader 99.00%
    RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections.
    RJS308 TFA
  • HY-186087
    RM-046
    		Ligand
    RM-046 is an orally active, selective ternary complex inhibitor of KRASQ61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRASQ61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRASQ61H mutant cancers.
    RM-046
  • HY-P11489
    RN-0001
    		Inhibitor
    RN-0001 is a cyclophilin (Cyp) inhibitor with Ki 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.
    RN-0001
  • HY-N0663
    Talatisamine
    		Activator 99.77%
    Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca2+-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC50=78 μM), and blocking delayed rectifier K+ channels (IC50=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.
    Talatisamine
  • HY-158409
    Pan-RAS-IN-2
    		99.74%
    Pan-rasin-2 (compound 6A) is an orally active molecular glues that targets RAS. Pan-RAS-IN-2 inhibits pERK (IC50 in AsPC-1 cells: 0.3 nM). Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor (such as colorectal cancer, pancreatic cancer) effects.
    Pan-RAS-IN-2
  • HY-107635
    TMN355
    		Inhibitor 99.67%
    TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis.
    TMN355
  • HY-112712
    Cyclophilin inhibitor 1
    		Inhibitor 99.55%
    Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
    Cyclophilin inhibitor 1
  • HY-135644
    Rencofilstat
    Rencofilstat (CRV431) is an orally active pan-cyclophilin inhibitor with IC50 values of 2.5 nM, 3.1 nM, 2.8 nM, 7.3 nM for Cyp A, CypB, Cyp D and Cyp G, respectively. Rencofilstat reduces fibrosis and tumor growth in models of chronic liver disease. Rencofilstat can be used for the study of nonalcoholic steatohepatitis (NASH), hepatocellular carcinoma and viral hepatitis-induced liver disease.
    Rencofilstat
  • HY-173011
    RJS308
    		Degrader 99.62%
    RJS308 is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 exhibits anti-HIV-1 and anti-HCV activities. RJS308 can be used in studies related to viral infections.
    RJS308
  • HY-129072
    Isocyclosporin A
    		99.05%
    Isocyclosporin A is a degradation product of the immunosuppressant Cyclosporin A.
    Isocyclosporin A
  • HY-157088
    C105SR
    		Inhibitor 99.49%
    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.
    C105SR
  • HY-P1355A
    Cyclosporin A-Derivative 1 Free base
    		98.20%
    Cyclosporin A-Derivative 1 (Free base) is a crystalline intermediate derived from the opening of cyclosporin A extracted from patent WO 2013167703 A1. Cyclosporin A is an immunosuppressive agent which can bind to the cyclophilin and inhibit calcineurin.
    Cyclosporin A-Derivative 1 Free base
  • HY-B0579S2
    Cyclosporin A acetate-d4
    		Inhibitor 99.90%
    Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium 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 also inhibits CD11a/CD18 adhesion.
    Cyclosporin A acetate-d<sub>4</sub>
  • HY-124072
    HL001
    		Inhibitor 98.90%
    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.
    HL001
  • HY-P1354
    Cyclosporin A-Derivative 2
    Cyclosporin A-Derivative 2 is a novel derivative from cyclosporin A. Cyclosporin A is an immunosuppressive agent which can bind to the cyclophilin and inhibit calcineurin.
    Cyclosporin A-Derivative 2
Cyclophilin Isoform Comparison

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