Cat. No.: HY-B0579

Cyclosporin A

(Synonyms: Cyclosporine A; Ciclosporin A; CsA)

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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.

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Pureté: 99.90%
CAS No.: 59865-13-3
Formule: C₆₂H₁₁₁N₁₁O₁₂
Masse moléculaire:1202.61

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Cyclosporin A Chemical Structure

CAS No.: 59865-13-3

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Description

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^[3]. 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^[8]^[9].

IC₅₀ & Target

Cyclophilin D

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Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	4.78 μM Compound: cyclosporin A	Inhibition of human MRP1 in human 2008 cells Inhibition of human MRP1 in human 2008 cells	[PMID: 18707884]
2008	IC₅₀	2.81 μM Compound: CsA	Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
2008	IC₅₀	2.7 μM Compound: Cyclosporine A	Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
A2780	IC₅₀	4.92 μM Compound: cyclosporin A	Inhibition of P-gp in human A2780 cells Inhibition of P-gp in human A2780 cells	[PMID: 18707884]
A2780	GI₅₀	8.94 μM Compound: Cyclosporine A	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780 ADR	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	[PMID: 19250834]
A2780 ADR	IC₅₀	0.99 μM Compound: CsA	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780 ADR	IC₅₀	0.92 μM Compound: Cyclosporine A	Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
A2780 ADR	IC₅₀	0.919 μM Compound: CsA	Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay	[PMID: 25855895]
A2780 ADR	GI₅₀	8.63 μM Compound: Cyclosporine A	Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780 ADR	IC₅₀	1.41 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay	[PMID: 27100033]
A2780 ADR	IC₅₀	1.21 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay	[PMID: 27676469]
B-cell	IC₅₀	0.07 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
B-cell	IC₅₀	0.159 μM Compound: CsA	Inhibition of LPS-induced BALB/c mouse B cell proliferation Inhibition of LPS-induced BALB/c mouse B cell proliferation	[PMID: 17081761]
B-cell	IC₅₀	0.74 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
Breast cancer cell line	EC₅₀	0.5 μM Compound: Cyclosporin A	Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%. Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.	[PMID: 11784143]
Breast cancer cell line	EC₅₀	0.6 μM Compound: Cyclosporin A	Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50% Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%	[PMID: 11784143]
Caco-2	IC₅₀	1.3 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 10820137]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 17936633]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 18257545]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells	[PMID: 18276145]
Caco-2	EC₅₀	45.5 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 18524592]
Caco-2	IC₅₀	2.9 μM Compound: CsA	Inhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux Inhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux	[PMID: 23382458]
Cancer cell lines	IC₅₀	1 μM Compound: Cyclosporin A	Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells. Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells.	[PMID: 11784143]
Cancer cell lines	IC₅₀	1.1 μM Compound: Cyclosporin A	Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells. Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells.	[PMID: 11784143]
CCRF-CEM	IC₅₀	3.4 μM Compound: 1	Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells	[PMID: 12361387]
CEM/VLB100	IC₅₀	3.41 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells	[PMID: 10891114]
EMT6	IC₅₀	440 nM Compound: Cyclosporin A	Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0 Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0	[PMID: 10098671]
HEK293	IC₅₀	1.3 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	37 μM Compound: Cyclosporin A	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	1.2 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HeLa	IC₅₀	1 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells	[PMID: 10565843]
HeLa	IC₅₀	>8.3 μM Compound: Cs	Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication	[PMID: 18212100]
HeLa	IC₅₀	6.6 μM Compound: Cs	Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days	[PMID: 18212100]
HepG2	IC₅₀	>50 μM Compound: 92125416	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	0.00165 μM Compound: 92125416	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HFF	IC₅₀	>10000 nM Compound: CSA	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
HL-60	IC₅₀	>10 μM Compound: 1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	[PMID: 12361388]
Huh-5-2	CC₅₀	6 μM Compound: Cyclosporine A	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	0.3 μM Compound: Cyclosporine A	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-5-2	CC₅₀	4.4 μM Compound: CsA	Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method	10.1039/C1MD00227A
Huh-5-2	EC₅₀	306 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay	10.1039/C1MD00227A
Huh-7	CC₅₀	5.62 μM Compound: CsA	Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 19933795]
Huh-7	EC₅₀	>10 μM Compound: CsA	Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	0.21 μM Compound: CsA	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	3.39 μM Compound: CsA	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	IC₅₀	5810 nM Compound: 1, CsA	Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase	[PMID: 20943390]
Huh-7	EC₅₀	137 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	198 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	455 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Jurkat	IC₅₀	>10 μM Compound: CsA	In vitro inhibition of Jurkat cell proliferation. In vitro inhibition of Jurkat cell proliferation.	[PMID: 11384243]
Jurkat	IC₅₀	>1 μM Compound: cyclosporin-A	Inhibition of production of beta-galactosidase thymidine kinase RGA in Jurkat cells Inhibition of production of beta-galactosidase thymidine kinase RGA in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	0.007 μM Compound: cyclosporin-A	Inhibition of production of IL-2 secretion in Jurkat cells Inhibition of production of IL-2 secretion in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	0.008 μM Compound: cyclosporin-A	Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	2 nM Compound: CsA	Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells. Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.	[PMID: 14643337]
Jurkat	EC₅₀	0.005 μM Compound: CsA	Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
Jurkat	EC₅₀	6.7 nM Compound: 1, CsA	Immunosuppressive activity against human Jurkat cells assessed as inhibition of phytohemagglutinin-M/phorbol myristate acetate-induced IL2 production Immunosuppressive activity against human Jurkat cells assessed as inhibition of phytohemagglutinin-M/phorbol myristate acetate-induced IL2 production	[PMID: 20943390]
Jurkat	IC₅₀	>10 μM Compound: CsA	Cytotoxicity against human Jurkat cells after 4 days by MTT assay Cytotoxicity against human Jurkat cells after 4 days by MTT assay	[PMID: 22984987]
Jurkat	IC₅₀	1.4 nM Compound: 1	Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay	[PMID: 23964991]
Jurkat	IC₅₀	11 nM Compound: 1; CyA	Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA	[PMID: 27647370]
Jurkat	IC₅₀	1.9 μM Compound: CsA	Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA	[PMID: 30579802]
Jurkat	IC₅₀	12 nM Compound: CsA	The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells. The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.	[PMID: 7473543]
Jurkat	IC₅₀	>10 μM Compound: CsA	In vitro inhibitory activity against Jurkat cell proliferation In vitro inhibitory activity against Jurkat cell proliferation	[PMID: 9719606]
Jurkat	IC₅₀	0.008 μM Compound: Cyclosporin A	Effect on the transcription and release of IL-2 in a reporter-gene assay (RGA) Effect on the transcription and release of IL-2 in a reporter-gene assay (RGA)	10.1016/S0960-894X(97)10005-1
K562/R7	IC₅₀	0.7 μM Compound: cyclosporin A	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay	[PMID: 25634041]
KB	IC₅₀	0.6 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB cell line after 72 h of drug exposure Inhibitory activity against KB cell line after 72 h of drug exposure	[PMID: 15481991]
KB 3-1	EC₅₀	1.2 μM Compound: CSA (cyclosporin A)	Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h	[PMID: 15481991]
KB 3-1	IC₅₀	1.5 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure	[PMID: 15481991]
KB 3-1	IC₅₀	23.9 μM Compound: Cyclosporine A	Cytotoxicity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Cytotoxicity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 35751979]
KB-V1	IC₅₀	7.95 μM Compound: Cyclosporine A	Cytotoxicity against human KB-V1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Cytotoxicity against human KB-V1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 35751979]
L929	IC₅₀	33.9 μM Compound: 2	Cytotoxicity against mouse L929 cells after 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs	[PMID: 22320402]
L929	IC₅₀	33.9 μM Compound: cyclosporine A	Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay	[PMID: 24171478]
L929	IC₅₀	30 μM Compound: cyclosporin A	Cytotoxicity against mouse L929 cells after 3 days by MTS assay Cytotoxicity against mouse L929 cells after 3 days by MTS assay	[PMID: 25985195]
L929	IC₅₀	29.9 μM Compound: Cyclosporin A	Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34597896]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	3.66 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 9914792]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay	[PMID: 20064721]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay	[PMID: 21171614]
Lymphocyte	EC₅₀	60 nM Compound: 1, CSA	Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay	[PMID: 24831536]
Lymphocyte	IC₅₀	89 nM Compound: CsA	Immunosuppressive activity in lymphocytes by MLR assay Immunosuppressive activity in lymphocytes by MLR assay	[PMID: 24900866]
Lymphocyte	CC₅₀	43.2 μM Compound: CsA	Cytotoxicity against lymphocytes (unknown origin) assessed as decrease in cell viability Cytotoxicity against lymphocytes (unknown origin) assessed as decrease in cell viability	[PMID: 29292227]
Lymphocyte	IC₅₀	0.2 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>9.9 μM Compound: Cs	Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK-II	IC₅₀	9.34 μM Compound: CsA	Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells	[PMID: 17664327]
MDCK-II	IC₅₀	13.6 μM Compound: cyclosporin A	Inhibition of human MRP2 expressed in dog MDCK2 cells Inhibition of human MRP2 expressed in dog MDCK2 cells	[PMID: 18707884]
MDCK-II	IC₅₀	25.6 μM Compound: Cyclosporine A	Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry	[PMID: 27393949]
MT4	IC₅₀	>0.83 μM Compound: Cs	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
MT4	EC₅₀	450 nM Compound: 1, CsA	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 23849880]
MT4	CC₅₀	5608 nM Compound: CSA	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay	[PMID: 30074795]
NCI/ADR-RES	IC₅₀	0.518 μM Compound: Cyclosporin A	Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay	[PMID: 36645980]
NCI/ADR-RES	IC₅₀	0.86 μM Compound: CyclosporinA	Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay	[PMID: 37229830]
NCI/ADR-RES	IC₅₀	0.29 μM Compound: Cyclosporin	Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM) Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM)	[PMID: 38364715]
Neutrophil	IC₅₀	0.047 nM Compound: CSA	Reduction of chemotaxis in human neutrophils assessed as inhibition of fMLP-OMe-induced cell migration pretreated 10 mins before fMLP-OMe challenge Reduction of chemotaxis in human neutrophils assessed as inhibition of fMLP-OMe-induced cell migration pretreated 10 mins before fMLP-OMe challenge	[PMID: 19362486]
NIH-3T3-G185	IC₅₀	1.4 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.7 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.7 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.1 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.4 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	4.3 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
PBMC	IC₅₀	12 nM Compound: cyclosporin A	Antiproliferative activity against human PBMC Antiproliferative activity against human PBMC	[PMID: 15679309]
PBMC	IC₅₀	0.056 μM Compound: Cs	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	EC₅₀	0.0031 μM Compound: CsA	Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
PBMC	IC₅₀	3 nM Compound: CsA	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
RD	CC₅₀	>10 μM Compound: CsA	Cytotoxicity against human RD cells after 24 hrs by WST-1 assay Cytotoxicity against human RD cells after 24 hrs by WST-1 assay	[PMID: 26564266]
RD	EC₅₀	3.66 μM Compound: CsA	Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay	[PMID: 26564266]
Sf21	IC₅₀	0.5 μM Compound: Cyclosporine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	0.6 μM Compound: Cyclosporine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Splenocyte	CC₅₀	0.88 μM Compound: CsA	Cytotoxicity against splenocytes after 48 hrs by MTT assay Cytotoxicity against splenocytes after 48 hrs by MTT assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in mouse splenocytes assessed as inhibition of allogenic mixed lymphocyte reaction Immunosuppressive activity in mouse splenocytes assessed as inhibition of allogenic mixed lymphocyte reaction	[PMID: 19502058]
Splenocyte	IC₅₀	10 nM Compound: Cyclosporine A	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	17 nM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	30 nM Compound: 1, CsA	Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay	[PMID: 23017885]
Splenocyte	IC₅₀	0.01 μg/mL Compound: Cyclosporine A	Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay	[PMID: 23167554]
Splenocyte	IC₅₀	0.1 μM Compound: Cyclosporin A	Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay	[PMID: 25537268]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay	[PMID: 30500185]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f	[PMID: 30500185]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte	[PMID: 30500185]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 31253536]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio	[PMID: 31253536]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc	[PMID: 31253536]
Splenocyte	IC₅₀	0.3 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33544615]
Splenocyte	IC₅₀	10.15 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 33973788]
Splenocyte	CC₅₀	>2.5 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 35104138]
Splenocyte	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.32 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	CC₅₀	7.33 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 35678710]
Splenocyte	EC₅₀	0.03 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay	[PMID: 36596229]
Splenocyte	CC₅₀	5.5 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes incubated for 48 hrs by MTT assay Cytotoxicity against BALB/c mouse splenocytes incubated for 48 hrs by MTT assay	[PMID: 37307145]
Splenocyte	IC₅₀	0.02 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of ConA-induced T cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of ConA-induced T cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis	[PMID: 37307145]
Splenocyte	IC₅₀	0.55 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-induced B cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-induced B cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis	[PMID: 37307145]
Splenocyte	IC₅₀	0.17 μM Compound: Cyclosporine A	Immunosuppressive activity in mouse splenocyte assessed as reduction in ConA-induced mouse T-cell proliferation Immunosuppressive activity in mouse splenocyte assessed as reduction in ConA-induced mouse T-cell proliferation	[PMID: 38128907]
Splenocyte	IC₅₀	0.07 μg/mL Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation	[PMID: 38441877]
T cell line	CC₅₀	9.8 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	IC₅₀	26 nM Compound: CsA	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation	[PMID: 11575965]
T-cell	IC₅₀	0.34 μM Compound: cyclosporin A	Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay	[PMID: 11678649]
T-cell	IC₅₀	32 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	74 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	>10000 nM Compound: CSA	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
T-cell	ED₅₀	50 nM Compound: Cyclosporin A	Inhibition of T-cell proliferation Inhibition of T-cell proliferation	[PMID: 15357990]
T-cell	IC₅₀	0.00137 μM Compound: CsA	Inhibition of ConA-induced BALB/c mouse T cell proliferation Inhibition of ConA-induced BALB/c mouse T cell proliferation	[PMID: 17081761]
T-cell	IC₅₀	550 nM Compound: CsA	Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting	[PMID: 19502058]
T-cell	CC₅₀	15.82 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	0.06 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	14 nM Compound: cyclosporin A	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay	[PMID: 21456524]
T-cell	IC₅₀	8.97 μM Compound: CYA	Inhibition of CD4 expression in human CD4+ T cells Inhibition of CD4 expression in human CD4+ T cells	[PMID: 22101135]
T-cell	CC₅₀	13.78 μM Compound: CsA	Cytotoxicity against lymph node T cell after 24 hrs by MTT assay Cytotoxicity against lymph node T cell after 24 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	2.12 μM Compound: csa	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay	[PMID: 22727369]
T-cell	IC₅₀	0.011 μM Compound: CsA	Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay	[PMID: 22984987]
T-cell	IC₅₀	0.57 μM Compound: CsA	Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation	[PMID: 26720154]
T-cell	EC₅₀	6.4 nM Compound: CsA	Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis	[PMID: 28075591]
T-cell	CC₅₀	4.5 μM Compound: Cyclosporin A	Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 28294615]
T-cell	IC₅₀	0.08 μM Compound: Cyclosporin A	Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method	[PMID: 28294615]
T-cell	IC₅₀	0.26 μM Compound: CsA	Inhibition of ConA-induced T lymphocytes (unknown origin) proliferation Inhibition of ConA-induced T lymphocytes (unknown origin) proliferation	[PMID: 29292227]
T-cell	IC₅₀	0.2 μM Compound: CsA	Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis	[PMID: 31181920]
T-cell	IC₅₀	0.1 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as reduction in ConA-induced cell proliferation Immunosuppressive activity in BALB/c mouse T cells assessed as reduction in ConA-induced cell proliferation	[PMID: 32323537]
T-cell	IC₅₀	0.046 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in guinea pig T cell assessed as inhibition of mitogenesis Immunosuppressive activity in guinea pig T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	0.28 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
T-cell	IC₅₀	1.05 μM Compound: Cyclosporine A	Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay	[PMID: 37017305]
T-cell	IC₅₀	13.7 nM Compound: CsA	In vitro inhibitory activity against human T-cell proliferation. In vitro inhibitory activity against human T-cell proliferation.	[PMID: 7537331]
T-cell	IC₅₀	8.1 nM Compound: CsA	In vitro inhibitory activity against human T-cell production of lymphokine IL-2 In vitro inhibitory activity against human T-cell production of lymphokine IL-2	[PMID: 7537331]
T-cell	IC₅₀	0.007 μM Compound: Cyclosporin A	Compound was tested for inhibition of IL-2 secretion in mouse T cell line Compound was tested for inhibition of IL-2 secretion in mouse T cell line	10.1016/S0960-894X(97)10005-1
Ventricular myocyte	IC₅₀	2 μM Compound: Cyclosporin A	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Vero	IC₅₀	>16.6 μM Compound: Cs	Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>25 μM Compound: Cs	Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>8.3 μM Compound: Cs	Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	8 μM Compound: Cs	Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	IC₅₀	≤0.5 μM Compound: Cs	Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	CC₅₀	>50 μM Compound: Cyclosporine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	5.82 μM Compound: Cyclosporine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Cyclosporin A is able to bind with the cyclophilin in T cells^[1].
Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin^[2].
Cyclosporin A inhibits calcineurin in stimulated cells with an IC₅₀ value of 7 nM^[3].
Cyclosporin A suppresses the nuclear translocation of NF-AT^[4].
Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC₅₀ of 39 nM^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Induced Disease Models

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Cyclosporin A can be used to construct uremia models. In male Wistar rats (weighing 140-200 g, aged 5-6 weeks), the pharmacokinetic parameters following intravenous administration of Cyclosporin A (10 mg/kg) show an area under the curve of 27.3 μg·h/mL, a half-life of 6.9 hours, and a volume of distribution of 3.7 L/kg^[9].

Induction of uraemia^[10]^[11]

Background

Cyclosporin A administration induces interstitial deposition of collagen type III and fibrosis via stimulation of the Transforming Growth Factor beta (TGF-β)-signalling pathway, while inhibiting extracellular matrix (ECM) degradation via modulation of matrix metallopeptidase 9, thus leading to an imbalance in ECM turn over^[2].

Specific Modeling Methods

Mice: Six-to-eight weeks old C57BL/6 mice
Administration: 30 mg/kg • SC • daily for 16 weeks

Note

Modeling Indicators

Molecular changes: Upregulated mRNA expression of both LOX, LOXL2, TNFα, MCP-1, (NOX)4; significantly downregulated SOD2 mRNA expression; increased the urea nitrogen (BUN) level, increased tubular injury, interstitial inflammation and fibrosis scores, PAS scores, increased the level the deposition of collagen type I (COL1) and type III (COL3) in the renal ECM,increased the expression of alpha-smooth-muscle actin (α-SMA), fibronectin (FN), COL1A, MCP-1^[10]^[11].

Opposite Product(s): Lipoxygenase, general (HY-P2976); Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11) (HY-P990107)

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 59865-13-3
Appearance Solid
Masse moléculaire 1202.61
Formule C₆₂H₁₁₁N₁₁O₁₂
Color White to off-white
SMILES

C/C=C/C[C@H]([C@@H](O)[C@@]1(N(C)C([C@]([H])(C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@]([H])(CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@@H](N(C([C@@]([H])(NC([C@@H](N(C(CN(C([C@@H](NC1=O)CC)=O)C)=O)C)CC(C)C)=O)C(C)C)=O)C)CC(C)C)=O)=O)=O)=O)=O)=O)[H])C
Synonyms

Cyclosporine A; Ciclosporin A; CsA
Structure Classification
- Others
Initial Source
- Microorganisms
the fungus Beauveria nivea.
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (213)

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Signal Transduct Target Ther

Targeting NFATc1-regulated MTHFD2 one-carbon metabolism to suppress sustained T-cell-mediated inflammation in rheumatoid arthritis. [Abstract]

2026 Jun 10;11(1):226. PMID: 42270592
Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Science

Zonated mechanosensing by PIEZO1 controls liver regeneration. [Abstract]

2026 Jul 2;393(6806):eaef0825. PMID: 42391361
Cell Metab

Hepatocyte-to-intestinal stem cell remote communication regulates blood glucose homeostasis. [Abstract]

2026 Jul 7;38(7):1367-1384.e9. PMID: 42309059
Cell Res

Transient mechanical activation of the Piezo1 channel facilitates ex vivo expansion of hematopoietic stem cells. [Abstract]

2026 Jan 9. PMID: 41507440
Nat Metab

Thermogenic adipocyte-derived zinc promotes sympathetic innervation in male mice. [Abstract]

2023 Mar;5(3):481-494. PMID: 36879120
Bioact Mater

Synergistic restoration of spinal cord injury through hyaluronic acid conjugated hydrogel-polydopamine nanoparticles combined with human mesenchymal stem cell transplantation. [Abstract]

2025 Feb 12:46:569-581. PMID: 40027446
Bioact Mater

cGAMP-targeting injectable hydrogel system promotes periodontal restoration by alleviating cGAS-STING pathway activation. [Abstract]

2025 Feb 13:48:55-70. PMID: 40303968
Bioact Mater

Engineered human spinal cord-like tissues with dorsal and ventral neuronal progenitors for spinal cord injury repair in rats and monkeys. [Abstract]

2023 Mar 29:27:125-137. PMID: 37064803
Bioact Mater

Transplantation of neural stem progenitor cells from different sources for severe spinal cord injury repair in rat. [Abstract]

2022 Nov 23:23:300-313. PMID: 36439085
Cell Stem Cell

Paired pre- and post-transplant human immunoprofiling identifies an IFN-γ-JAK1 axis limiting stem-cell-derived RPE engraftment. [Abstract]

2026 Jul 2;33(7):1127-1143.e10. PMID: 42309064
Autophagy

Mechanical stress-mediated ferritinophagy aggravates cartilage endplate degeneration via a PIEZO1-NCOA4-ZBP1 axis. [Abstract]

2026 May 31:1-22. PMID: 42153663
Autophagy

Impaired mitophagy contributes to osteogenesis and mineralization disorders in fibrous dysplasia. [Abstract]

2026 Mar 15:1-22. PMID: 41803635
Protein Cell

Spatiotemporal Ca2+ nanodomain remodeling at MERCS regulates mitochondrial proteostasis. [Abstract]

2025 Dec 8:pwaf109. PMID: 41359778
Nat Commun

Helicobacter hepaticus promotes hepatic steatosis through CdtB-induced mitochondrial stress and lipid metabolism reprogramming. [Abstract]

2025 Aug 26;16(1):7954. PMID: 40858606
Nat Commun

Endothelial major vault protein alleviates vascular remodeling via promoting Parkin-mediated mitophagy. [Abstract]

2025 May 10;16(1):4365. PMID: 40348769
Nat Commun

Heterozygous de novo dominant negative mutation of REXO2 results in interferonopathy. [Abstract]

2024 Aug 6;15(1):6685. PMID: 39107301
Nat Commun

Perfluoroalkyl substance pollutants activate the innate immune system through the AIM2 inflammasome. [Abstract]

2021 May 18;12(1):2915. PMID: 34006824

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915. [Abstract]

Immunoblot analysis of Cytochrome c from cytosolic extracts and mitochondria from indicated cells pre-treated with DMSO or Cyclosporine A (50 μM) for 1 h, followed with PFOS treatment (150 μM, 6 h).

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 May 18;12(1):2915. [Abstract]

THP-1-derived macrophages were treated with DMSO or cyclosporine A (50 μM) for 1 h followed by PFOS (150 μM, 6 h), poly (dA:dT) (2 μg/ml, 6 h) treatment or pre-treated with LPS (200 ng/ml, 3 h) followed ATP (5 mM, 6 h) treatment.
Exp Mol Med

Cytosolic escape of mitochondrial DNA triggers cGAS-STING-NLRP3 axis-dependent nucleus pulposus cell pyroptosis. [Abstract]

2022 Feb;54(2):129-142. PMID: 35145201

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]

Representative western blotting images of cGAS and STING in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]

Representative immunofluorescence images of STING with different degrees of polymerization in the Cyclosporine (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2022 Feb;54(2):129-142. [Abstract]

Representative western blotting images of NLRP3, ASC, pro-CASP-1, cleaved CASP-1, GSDMD, and cleaved GSDMD in the (CsA; 10 μM; for 24 h)- or DMSO-treated NP cells.
ACS Nano

Programmed Cell Death Protein 1 Engagement Impairs Cytoskeletal Forces and Nuclear Mechanotransduction in T Cells. [Abstract]

2025 Nov 25;19(46):39667-39681. PMID: 41221724
J Adv Res

Conjugated bile acids facilitate cholangiocyte senescence to promote cholestatic liver diseases via STING signaling. [Abstract]

2026 Mar 12:S2090-1232(26)00239-0. PMID: 41831676
Redox Biol

Histidine metabolic reprogramming drives oxidative stress induced mtDNA release to promote necroptosis and airway inflammation in severe asthma. [Abstract]

2026 Jun 27:95:104280. PMID: 42372708
Redox Biol

Extracellular vesicle-mediated delivery of mitochondrial circRNA MTCO2 protects against cerebral ischemia by modulating mPTP-dependent ferroptosis. [Abstract]

2025 Aug 5:86:103806. PMID: 40768899
Redox Biol

CypD induced ROS output promotes intracranial aneurysm formation and rupture by 8-OHdG/NLRP3/MMP9 pathway. [Abstract]

2023 Nov:67:102887. PMID: 37717465
Redox Biol

Cationic antimicrobial peptide NRC-03 induces oral squamous cell carcinoma cell apoptosis via CypD-mPTP axis-mediated mitochondrial oxidative stress. [Abstract]

2022 Aug;54:102355. PMID: 35660629

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355. [Abstract]

Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). Cell viability determined by CCK-8.

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Redox Biol. 2022 Aug;54:102355. [Abstract]

Cells are treated with or without Cyclosporine A (CsA; 2 μM) for 4 h in presence of NRC-03 (45 μg/mL). TUNEL immunofluorescence staining and quantification of TUNEL positive cells.
J Nanobiotechnology

Ag2Se quantum dots neurotoxicity: mitochondrial stress drives ferroptosis-dependent microglial inflammation. [Abstract]

2026 Apr 2;24(1):431. PMID: 41928263
Theranostics

Reprogramming Exosomes to Escape from Immune Surveillance for Mitochondrial Protection in Hepatic Ischemia-Reperfusion Injury. [Abstract]

2024 Jan 1;14(1):116-132. PMID: 38164154
Acta Pharm Sin B

Generation and applications of an expandable and mature hiPSC-derived liver organoid. [Abstract]

2025 Dec;15(12):6382-6398. PMID: 41477334
Adv Sci (Weinh)

NADH-Reductive Stress Induced by Dihydrolipoamide Dehydrogenase Activation Contributes to Cuproptosis. [Abstract]

2025 Dec 5:e20444. PMID: 41346305
Adv Sci (Weinh)

LPS-Induced Mitochondrial Damage via SLC41A1-Mediated Magnesium Ion Efflux Leads to the Pyroptosis of Dental Stem Cells. [Abstract]

2025 Aug 19:e05666. PMID: 40831212
Adv Sci (Weinh)

Mesenchymal Stem Cell Membrane-Camouflaged Liposomes for Biomimetic Delivery of Cyclosporine A for Hepatic Ischemia-Reperfusion Injury Prevention. [Abstract]

2024 Jun 20:e2404171. PMID: 39031840

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 20:e2404171. [Abstract]

Cell viability of H/R‐injured cells after being treated with free CsA, CLs, and MMCLs at CsA concentrations of 0 − 500 ng/mL as evaluated by CCK‐8 assay.
Adv Sci (Weinh)

Glutamine Metabolism Underlies the Functional Similarity of T Cells between Nile Tilapia and Tetrapod. [Abstract]

2023 Apr;10(12):e2201164. PMID: 36890649

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Apr;10(12):e2201164. [Abstract]

Relative mRNA levels of indicated molecules in spleen leukocytes. N) Healthy tilapia were injected with 293T cells on day 1 and 3, and treated with 10 mg/kg Cyclosporine A (CyA) on day 1, 3, and 5. Spleen T cells were sorted on day 6 and incubated with 293T or NIH3T3 cells for 8 h, and LDH release was detected.
Adv Sci (Weinh)

MCU Upregulation Overactivates Mitophagy by Promoting VDAC1 Dimerization and Ubiquitination in the Hepatotoxicity of Cadmium. [Abstract]

2023 Mar;10(7):e2203869. PMID: 36642847
Adv Sci (Weinh)

Mitochondrial Damage-Induced Innate Immune Activation in Vascular Smooth Muscle Cells Promotes Chronic Kidney Disease-Associated Plaque Vulnerability. [Abstract]

2021 Jan 6;8(5):2002738. PMID: 33717842
Sci Adv

Spinal cord tissue engineering via covalent interaction between biomaterials and cells. [Abstract]

2023 Feb 10;9(6):eade8829. PMID: 36753555
Cell Death Differ

Efferocytosis enhances macrophage pro-angiogenic functions for bone marrow regeneration. [Abstract]

2026 Jun 24. PMID: 42337094
Research (Wash D C)

Extracellular Vesicle-Mediated Delivery of Mitochondrial Circular RNA MTCO2 Protects against Cerebral Ischemia by Modulating mPTP-Dependent Ferroptosis. [Abstract]

2026 Apr 14:9:1232. PMID: 41988019
Research (Wash D C)

Mitochondrial 8-Oxoguanine DNA Glycosylase 1-Mitochondrial Permeability Transition Pore Axis Drives Mitochondrial DNA Escape and Accelerates Osteoarthritis Progression. [Abstract]

2026 Apr 15:9:1235. PMID: 41993093
Pharmacol Res

SERCA2 dysfunction drives vascular calcification via coupling with TSPO-MCU at mitochondria-associated endoplasmic reticulum membranes. [Abstract]

2026 May:227:108177. PMID: 41932666
Cell Death Dis

Generation of proliferative hESC-derived grape-clustered hepatocyte organoids with multipolar architecture as regenerative counterpart via synergy of YAP and IGF2 pathways. [Abstract]

2026 Mar 26;17(1):381. PMID: 41888105
Cell Death Dis

Mitochondrial DNA drives NLRP3-IL-1β axis activation in microglia by binding to NLRP3, leading to neurodegeneration in Parkinson's disease models. [Abstract]

2026 Feb 10;17(1):213. PMID: 41667433
Pharmacol Res

Microglia sense and suppress epileptic neuronal hyperexcitability. [Abstract]

2023 Sep:195:106881. PMID: 37541638
Cell Death Dis

RANK promotes colorectal cancer migration and invasion by activating the Ca2+-calcineurin/NFATC1-ACP5 axis. [Abstract]

2021 Apr 1;12(4):336. PMID: 33795653

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 1;12(4):336. [Abstract]

Immunofluorescence staining of subcellular localization of NFATC1 in RANK overexpression and control cells with or without treatment of 10 μg/mL Cyclosporin A (CsA).
Cell Death Dis

Mitochondrial quality control protects photoreceptors against oxidative stress in the H2O2-induced models of retinal degeneration diseases. [Abstract]

2021 Apr 20;12(5):413. PMID: 33879768

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Apr 20;12(5):413. [Abstract]

Inhibition of NR-induced increase of co-localized puncta (LC3 and TOM20) after 1 μMCyclosporin A (CsA) pretreatment.
Cell Death Dis

Hirsutine induces mPTP-dependent apoptosis through ROCK1/PTEN/PI3K/GSK3β pathway in human lung cancer cells. [Abstract]

2018 May 22;9(6):598. PMID: 29789524

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):598. [Abstract]

A549 cells are pretreated with 5 µM Cyclosporin A (CSA) for 2 h, followed by treatment with 80 μM Hirsutine for 24 h. equal amount of lysates are subjected to immunoprecipitation using anti-ANT1 antibody, the associated CypD is determined using immunoblotting.
Environ Sci Technol

Determining the Cytotoxicity of Rare Earth Element Nanoparticles in Macrophages and the Involvement of Membrane Damage. [Abstract]

2017 Dec 5;51(23):13938-13948. PMID: 29121463
Cell Commun Signal

Mitochondrial DNA release via mPTP and BAX/BAK drives inflammatory injury in intestinal ischemia reperfusion. [Abstract]

2025 Dec 24;24(1):50. PMID: 41437056
Cell Commun Signal

IRF1 regulation of ZBP1 links mitochondrial DNA and chondrocyte damage in osteoarthritis. [Abstract]

2024 Jul 18;22(1):366. PMID: 39026271
Phytomedicine

Lithospermic acid alleviates myocardial ischemia/reperfusion injury by inhibiting mitophagy via the Piezo1-PPP3/calcineurin-TFEB pathway. [Abstract]

2025 Oct 11:148:157402. PMID: 41101069
Adv Healthc Mater

Adaptable Covalent Organic Framework-Hydrogel Microneedles for Glucose-Responsive Isoliquiritigenin Delivery in Diabetic Wound Therapy. [Abstract]

2026 Jul;15(26):e71343. PMID: 42277632
Mater Today Bio

Ultrasound-driven microbubble motors for targeted myocardial ischemia-reperfusion injury treatment. [Abstract]

2026 Jun 13:39:103349. PMID: 42368711
Mater Today Bio

Early-apoptotic membrane engineering of M2 macrophage-derived nanovesicles enables osteoimmunomodulatory bone repair. [Abstract]

2026 Jun 8:38:103324. PMID: 42293395
Appl Phys Rev

2026 Jan 21.
Acta Pharmacol Sin

Baicalin inhibits PANoptosis by blocking mitochondrial Z-DNA formation and ZBP1-PANoptosome assembly in macrophages. [Abstract]

2025 Feb;46(2):430-447. PMID: 39223367
Arthritis Rheumatol

mTOR inhibition prevents coronary artery remodeling in a murine model of Kawasaki disease. [Abstract]

2023 Feb;75(2):305-317. PMID: 36057112
Biomater Res

Distinct Roles of Matrigel Enabled the Production of Expandable Hepatoblast and Polarized Hepatocyte Organoids from Human Embryonic Stem Cells under 3-Dimensional Suspension Conditions. [Abstract]

2025 Nov 7:29:0280. PMID: 41209312
J Transl Med

MPTP mediated Ox-mtDNA release inducing macrophage pyroptosis and exacerbating MCD-induced MASH via promoting the ITPR3/Ca2+/NLRP3 pathway. [Abstract]

2025 Nov 14;23(1):1289. PMID: 41239426
J Transl Med

Blockade of the mitochondrial DNA release ameliorates hepatic ischemia-reperfusion injury through avoiding the activation of cGAS-Sting pathway. [Abstract]

2024 Aug 28;22(1):796. PMID: 39198913
Sci China Life Sci

Spinal segment-specific properties of neural stem cells contribute to the outcomes of spinal cord injury repair. [Abstract]

2025 Aug 22. PMID: 40856925
Aging Dis

P-Glycoprotein Aggravates Blood Brain Barrier Dysfunction in Experimental Ischemic Stroke by Inhibiting Endothelial Autophagy. [Abstract]

2022 Oct 1;13(5):1546-1561. PMID: 36186136

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Aging Dis. 2022 Oct 1;13(5):1546-1561. [Abstract]

Additionally, similar to P-gp siRNA silence, pharmacological inhibition of P-gp with Cyclosporine A (CsA; 22 mg/kg) significantly attenuates P-gp expression levels in ischemic brain as compared to vehicle treatment.
Proc Natl Acad Sci U S A

Calcineurin controls proximodistal blastema polarity in zebrafish fin regeneration. [Abstract]

2021 Jan 12;118(2):e2009539118. PMID: 33376206

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118. [Abstract]

Calcineurin activities of the PCE after FK506 or Cyclosporine A (CsA; 4 µM) treatment Zebrafish.
Oncogene

CypA/TAF15/STAT5A/miR-514a-3p feedback loop drives ovarian cancer metastasis. [Abstract]

2024 Nov;43(49):3570-3585. PMID: 39402372
Cell Chem Biol

In vivo drug discovery for increasing incretin-expressing cells identifies DYRK inhibitors that reinforce the enteroendocrine system. [Abstract]

2022 Sep 15;29(9):1368-1380.e5. PMID: 35998625
Int J Biol Macromol

Cordyceps militaris polysaccharide converts immunosuppressive macrophages into M1-like phenotype and activates T lymphocytes by inhibiting the PD-L1/PD-1 axis between TAMs and T lymphocytes. [Abstract]

2020 May 1;150:261-280. PMID: 32044366
Int J Mol Med

Human papillomavirus E7 inhibits immune responses in keratinocytes by activating HTRA1‑mediated mitophagy. [Abstract]

2026 Jan;57(1):22. PMID: 41235661
Neural Regen Res

Cyclophilin D-induced mitochondrial impairment confers axonal injury after intracerebral hemorrhage in mice. [Abstract]

2023 Apr;18(4):849-855. PMID: 36204853
Int J Mol Med

TRAP1 attenuates H9C2 myocardial cell injury induced by extracellular acidification via the inhibition of MPTP opening. [Abstract]

2020 Aug;46(2):663-674. PMID: 32626957
EMBO J

NRF1-mediated mitochondrial biogenesis antagonizes innate antiviral immunity. [Abstract]

2023 Aug 15;42(16):e113258. PMID: 37409632
Antioxidants (Basel)

Reactive Oxygen Species Damage Bovine Endometrial Epithelial Cells via the Cytochrome C-mPTP Pathway. [Abstract]

2023 Dec 16;12(12):2123. PMID: 38136242
Antioxidants (Basel)

Muscone and (+)-Borneol Cooperatively Strengthen CREB Induction of Claudin 5 in IL-1 β-Induced Endothelium Injury. [Abstract]

2022 Jul 26;11(8):1455. PMID: 35892657
Free Radic Biol Med

Echinacoside improves antioxidant responses and angiogenesis through Parkin-MFN2-mediated mitophagy to promote diabetic wound healing. [Abstract]

2026 Jul:250:436-452. PMID: 41962601
Free Radic Biol Med

LL37-induced mitochondrial stress activates the mtDNA/cGAS/STING pathway to promote mast cell-mediated rosacea inflammation. [Abstract]

2025 Dec 18:244:422-434. PMID: 41421415
Free Radic Biol Med

Redox switch C674 in SERCA2 triggers Ca2+-calcineurin-MCU-Drp1 cascade and pulmonary vascular remodeling. [Abstract]

2025 Dec 16:244:380-394. PMID: 41412527
Free Radic Biol Med

LINC03047 promotes mitophagy by recruiting hnRNPF to enhance CTGF mRNA stability in hypoxic pulmonary hypertension. [Abstract]

2025 Nov 11:243:111-125. PMID: 41232621
Free Radic Biol Med

2025 Oct 25.
Free Radic Biol Med

Calcineurin/NFAT1/Smad2 signaling regulates microglial autophagy that contributes to neuroinflammation and cognitive deficit in mice with sepsis-associated encephalopathy. [Abstract]

2025 Aug 8:240:15-28. PMID: 40784585
Free Radic Biol Med

The tolerable upper intake level of manganese alleviates Parkinson-like motor performance and neuronal loss by activating mitophagy. [Abstract]

2024 Nov 20:225:665-676. PMID: 39401732
Free Radic Biol Med

Exosomes derived from schwann cells alleviate mitochondrial dysfunction and necroptosis after spinal cord injury via AMPK signaling pathway-mediated mitophagy. [Abstract]

2023 Nov 1:208:319-333. PMID: 37640169
Int J Pharm X

Ultrasound-targeted sirolimus-loaded microbubbles improves acute rejection of heart transplantation in rats by inhibiting TGF-β1-Smad signaling pathway, promoting autophagy and reducing inflammation. [Abstract]

2024 Nov 4:8:100300. PMID: 39624342
Clin Transl Med

Translocation of gasdermin D induced mitochondrial injury and mitophagy mediated quality control in lipopolysaccharide related cardiomyocyte injury. [Abstract]

2022 Aug;12(8):e1002. PMID: 36030524
Stem Cell Res Ther

hPSC-derived sacral neural crest cells restore erectile function in pelvic ganglia injury. [Abstract]

2025 Oct 29;16(1):593. PMID: 41163062
Cell Rep

Fibroblast MrgprX2/B2 signaling drives hypertrophic scar fibrosis. [Abstract]

2026 Jun 25;45(7):117616. PMID: 42360879
Cell Rep

STING-OPTN signaling confers cytoprotection through TBK1-dependent mitophagy. [Abstract]

2026 Jun 9;45(6):117515. PMID: 42268710
Cell Rep

Aryl hydrocarbon receptor-induced activation of AIM2 inflammasome is mediated by MOMP and MPT: A vital therapeutic pathway for inflammation. [Abstract]

2025 Dec 10;44(12):116673. PMID: 41385364
Cell Rep

Stem cell differentiation with consistent lineage commitment induced by a flash of ultrafast-laser activation in vitro and in vivo. [Abstract]

2022 Mar 8;38(10):110486. PMID: 35263591
Cell Rep

Redox-sensitive cyclophilin A elicits chemoresistance through realigning cellular oxidative status in colorectal cancer. [Abstract]

2021 Nov 30;37(9):110069. PMID: 34852234

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]

Colony formation of CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA for 48 h.

Cyclosporin A purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Nov 30;37(9):110069. [Abstract]

Immunoblotting analysis of indicated apoptotic markers expression in CRC cells treated with Cyclosporine A (CsA; 2.5-5 μM) in combination with 5-FU or OXA.
Cell Rep

Neuronal activity recruits the CRTC1/CREB axis to drive transcription-dependent autophagy for maintaining late-phase LTD. [Abstract]

2021 Jul 20;36(3):109398. PMID: 34289350
Cell Prolif

Establishment of human corneal epithelial organoids for ex vivo modelling dry eye disease. [Abstract]

2024 Jul 3:e13704. PMID: 38961590
Br J Pharmacol

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Br J Pharmacol

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Cyclosporin A purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Jun;178(11):2305-2323. [Abstract]

Smooth muscle cells are treated cyclosporin A (CsA, 1 μM) or PDTC (10 μM) for 24 h before measuring the activity of PPARγ2 promoter.
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Modelling the maternal-fetal interface: An in vitro approach to investigate nutrient and drug transport across the human placenta. [Abstract]

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2022 Jan;160(1):51-63. PMID: 34407220
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2025 Jan 16:111214. PMID: 39826756
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2024 Aug 22;27(10):110784. PMID: 39391723
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Umbilical cord mesenchymal stem cell-conditioned medium inhibits microglial activation to ameliorate neuroinflammation in amyotrophic lateral sclerosis mice and cell models. [Abstract]

2023 Oct 1:202:110760. PMID: 37704056
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Induction of multiple subroutines of regulated necrosis in murine macrophages by natural BH3-mimetic gossypol. [Abstract]

2022 Jan 25;54(1):64-76. PMID: 35130622
ACS Chem Neurosci

Short-Term Extremely Low-Frequency Electromagnetic Field Inhibits Synaptic Plasticity of Schaffer Collateral-CA1 Synapses in Rat Hippocampus via the Ca2+/Calcineurin Pathway. [Abstract]

2021 Oct 6;12(19):3550-3557. PMID: 34498467
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Penicillide Triggers Immunogenic Pyroptosis in Tumor Cells via Oxidative Stress/NF-κB/GSDMD Signaling Axis. [Abstract]

2026 Mar 31;40(6):e71636. PMID: 41842655
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ORAI3 Modulates Oral Squamous Cell Carcinoma Metastasis Through the Ca2+/Calmodulin/Calcineurin/ETV4 Signaling Pathway. [Abstract]

2025 Dec 31;39(24):e71322. PMID: 41417281
FEBS J

Oxaliplatin accelerates immunogenic cell death by activating the cGAS/STING/TBK1/IRF5 pathway in gastric cancer. [Abstract]

2025 Apr 22. PMID: 40260556
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Cyclophilin A facilitates HIV-1 integration. [Abstract]

2024 Nov 19;98(11):e0094724. PMID: 39480090
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Cytomegalovirus infection initiates inflammatory bowel disease by activating a positive MyD88/NF-κB feedback loop in allogeneic skin transplantation mice. [Abstract]

2025 Apr 16;22(1):101. PMID: 40241182
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Kaempferol attenuates cyclosporine-induced renal tubular injury via inhibiting the ROS-ASK1-MAPK pathway. [Abstract]

2025 Mar;398(3):3001-3014. PMID: 39316086
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IL-2 Signaling Couples the MAPK and mTORC1 Axes to Promote T Cell Proliferation and Differentiation in Teleosts. [Abstract]

2022 Apr 1;208(7):1616-1631. PMID: 35321881
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Ca2+-Calcineurin Axis-Controlled NFAT Nuclear Translocation Is Crucial for Optimal T Cell Immunity in an Early Vertebrate. [Abstract]

2020 Feb 1;204(3):569-585. PMID: 31871019
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Effects of Destruxin A on Silkworm's Immunophilins. [Abstract]

2019 Jun 18;11(6):349. PMID: 31216655
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2024 Aug.
Neurotox Res

Apelin-36 Protects HT22 Cells Against Oxygen-Glucose Deprivation/Reperfusion-Induced Oxidative Stress and Mitochondrial Dysfunction by Promoting SIRT1-Mediated PINK1/Parkin-Dependent Mitophagy. [Abstract]

2021 Jun;39(3):740-753. PMID: 33580874
Vet Res

Residue 188 of the Hexon protein governs FAdV-4 pathogenicity by activating PINK1/Parkin-mediated mitophagy. [Abstract]

2026 Jun 13;57(1):107. PMID: 42288922
ESC Heart Fail

Inhibition of adenosine kinase alleviates hypertrophic cardiomyopathy by ameliorating coronary microvascular dysfunction. [Abstract]

2026 May 5;13(3):xvag118. PMID: 42015547
Viruses

Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]

2020 Jun 10;12(6):628. PMID: 32532085
Biochim Biophys Acta Mol Cell Biol Lipids

Macrophage iron retention aggravates atherosclerosis: Evidence for the role of autocrine formation of hepcidin in plaque macrophages. [Abstract]

2020 Feb;1865(2):158531. PMID: 31666189
Mol Immunol

Gelatin enhances bacteria-phagocytosis via a ROS-mitochondria-STING axis in differentiated human macrophage-like U937 cells. [Abstract]

2025 Oct:186:48-62. PMID: 40815890
Drug Metab Dispos

Activation of pregnane X receptor-organic anion transporting polypeptide 1a/b /P-glycoprotein/multidrug resistance protein 2 axis mediates the accelerated blood and liver clearance of PEGylated liposomes. [Abstract]

2025 Nov;53(11):100172. PMID: 41106060
Drug Metab Dispos

Unveiling hepatic Krüppel-like factor 15 as the key regulator of cyclosporine A metabolism and adverse effects. [Abstract]

2025 Jul 29;53(9):100136. PMID: 40885107
Drug Metab Dispos

Identification of selective substrates and inhibitors of the major human renal uptake transporters. [Abstract]

2025 Mar;53(3):100046. PMID: 40024137
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
J Radiat Res Appl Sci

2026 Feb 24.
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Mycoplasma pneumoniae-induced Kawasaki disease via PINK1/Parkin-mediated mitophagy. [Abstract]

2024 Jul 31;441(2):114182. PMID: 39094903
Arch Biochem Biophys

Silibinin alleviates ferroptosis of rat islet β cell INS-1 induced by the treatment with palmitic acid and high glucose through enhancing PINK1/parkin-mediated mitophagy. [Abstract]

2023 Jul 15:743:109644. PMID: 37245586
J Neurooncol

Single-cell RNA-seq reveals diverse molecular signatures associated with Methotrexate resistance in primary central nervous system lymphoma cells. [Abstract]

2025 Mar;172(1):163-173. PMID: 39636551
Phytochemistry

Immunosuppressive gentianellane-type sesterterpenoids from the traditional Uighur medicine Gentianella turkestanorum. [Abstract]

2021 Jul:187:112780. PMID: 33915419
Neuroscience

Trichostatin A-primed spinal cord organoids alleviate oxidative stress and improve recovery after spinal cord injury involving the NRF2/HO-1 signaling pathway. [Abstract]

2026 Jun 6:610:122-135. PMID: 42250855
Int J Cardiol

Kirenol attenuates pressure overload-induced heart failure by enhancing autophagy in macrophages. [Abstract]

2025 Dec 1:440:133681. PMID: 40752803
Food Chem Toxicol

Ginsenoside Rb1 alleviates 3-MCPD-induced renal cell pyroptosis by activating mitophagy. [Abstract]

2024 Apr:186:114522. PMID: 38373586
Food Chem Toxicol

Alliin alleviates LPS-induced pyroptosis via promoting mitophagy in THP-1 macrophages and mice. [Abstract]

2022 Feb:160:112811. PMID: 34999177
Kaohsiung J Med Sci

Melatonin Exerts Chondroprotective Effects Against Osteoarthritis by Promoting PI3K/AKT/FoxO3-Mediated Mitophagy. [Abstract]

2025 Nov 5:e70131. PMID: 41190713
BMC Cardiovasc Disord

Calcineurin/NFATc3 pathway mediates myocardial fibrosis in diabetes by impairing enhancer of zeste homolog 2 of cardiac fibroblasts. [Abstract]

2023 Sep 21;23(1):474. PMID: 37735624
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Cyclosporin A alleviates trophoblast apoptosis and senescence by promoting autophagy in preeclampsia. [Abstract]

2022 Jan:117:95-108. PMID: 34785431
Cell Biochem Biophys

Downregulation of IGFBP7 Alleviates LPS-induced Inflammation and Apoptosis in WI-38 Cells via Enhancing Mitophagy. [Abstract]

2025 Jun;83(2):1565-1573. PMID: 39347911
Vet Microbiol

Cytopathic BVDV engages VDAC1 through NS3 to trigger mitochondrial permeability transition-dependent intrinsic apoptosis. [Abstract]

2026 Aug:319:111069. PMID: 42139791
Toxicol In Vitro

Clarify the potential cholestatic hepatotoxicity components from Chinese Herb Medicine and metabolism's role via hBSEP vesicles and S9/hBSEP vesicles. [Abstract]

2022 Apr:80:105324. PMID: 35101544
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Host defense peptide Hymenochirin-1B induces lung cancer cell apoptosis and cell cycle arrest through the mitochondrial pathway. [Abstract]

2019 Apr 30;512(2):269-275. PMID: 30885438
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Effects of intracellular iron overload on cell death and identification of potent cell death inhibitors. [Abstract]

2018 Sep 3;503(1):297-303. PMID: 29890135
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The Differential Effects of Immunosuppressants on Hepatitis E Virus Replication and the Triggered Inflammatory Responses in Macrophages. [Abstract]

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PROSER2 is a poor prognostic biomarker for patients with osteosarcoma and promotes proliferation, migration and invasion of osteosarcoma cells. [Abstract]

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Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells. [Abstract]

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Establishment of a novel myocarditis mouse model based on cyclosporine A. [Abstract]

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Collagen I alleviates UVB-induced oxidative DNA damage and inhibits YAP-p73 apoptotic pathway in human keratinocytes HaCaT. [Abstract]

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Increased GABBR2 Expression on Cell Membranes Causes Increased Ca2 + Inward Flow, Associated with Cognitive Impairment in Early Alzheimer's Disease. [Abstract]

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Solvant et solubilité

In Vitro:

DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8315 mL

4.1576 mL

8.3152 mL

5 mM

0.1663 mL

0.8315 mL

1.6630 mL

10 mM

0.0832 mL

0.4158 mL

0.8315 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[3]

Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (10⁶) are suspended in 1 mL of complete medium in microcentrifuge tubes; 1 μL of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 mL of PBS on ice and lysed in 50 μL of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of Kiker 52G per mL. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[6]

Rats are immunized on day 0 i.p. with 0 5 mL and mice i.v. with 0 2 mL of a 10% suspension of washed sheep erythrocytes (SE). To elicit a secondary response, mice are boosted 8-11 weeks after the primary immunization with an i.v. injection of 0-2 mL of 0 25% washed SE (10⁷ cells). For prolonged treatment the animals receive on the average 45 mg/kg cyclosporin A daily in the food during 13 weeks. These rats are immunized 5 days before killing.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (294 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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OR (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief]

[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief]

[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief]

[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief]

[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92. [Content Brief]

[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief]

[7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief]

[8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief]

[9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief]

[10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief]

[11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

[12]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	0.8315 mL	4.1576 mL	8.3152 mL	20.7881 mL
	5 mM	0.1663 mL	0.8315 mL	1.6630 mL	4.1576 mL
	10 mM	0.0832 mL	0.4158 mL	0.8315 mL	2.0788 mL
	15 mM	0.0554 mL	0.2772 mL	0.5543 mL	1.3859 mL
	20 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0394 mL
	25 mM	0.0333 mL	0.1663 mL	0.3326 mL	0.8315 mL
	30 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6929 mL
	40 mM	0.0208 mL	0.1039 mL	0.2079 mL	0.5197 mL
DMSO	50 mM	0.0166 mL	0.0832 mL	0.1663 mL	0.4158 mL

Keywords

Cyclosporin A

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Cyclosporin A

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