| S1322 |
Dexamethasone
|
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
-
Signal Transduct Target Ther, 2025, 10(1):230
-
Signal Transduct Target Ther, 2025, 10(1):394
-
Gut, 2025, gutjnl-2025-336105
|
|
| S2286 |
Cyclosporin A
|
Cyclosporin A, a non-polar cyclic oligopeptide, is an immunosuppressive agent that binds to cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay. Cyclosporin A is generally given following transplant surgery to prevent rejection and has been used to test its toxic effect on a perfused 3D proximal tubule model.Cyclosporin A (NSC 290193) can be used to induce animal models of Chronic Rejection of Liver Transplantation. |
-
Signal Transduct Target Ther, 2025, 10(1):81
-
Signal Transduct Target Ther, 2025, 10(1):167
-
Adv Sci (Weinh), 2025, 12(36):e06150
|
|
| S3124 |
Dexamethasone Acetate
|
Dexamethasone (NSC 39471,Dexamethasone 21-acetate) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
-
Acta Pharm Sin B, 2024, 14(8):3528-3542
-
STAR Protoc, 2023, 4(2):102342
-
Exp Mol Med, 2022, 54(9):1450-1460
|
|
| S4028 |
Dexamethasone Sodium Phosphate
|
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
-
Proc Natl Acad Sci U S A, 2025, 122(12):e2426107122
-
J Tradit Chin Med, 2025, 45(4):739-746
-
Cancer Cell, 2024, 42(9):1507-1527.e11
|
|
| S8522 |
Compstatin
|
Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. |
-
Nat Commun, 2025, 16(1):2493
-
Proc Natl Acad Sci U S A, 2025, 122(20):e2412447122
-
CNS Neurosci Ther, 2025, 31(1):e70216
|
|
| S8306 |
Leukadherin-1
|
Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)). |
-
International Immunopharmacology, 2023, Volume 118
-
Int Immunopharmacol, 2023, 118:110024
-
Front Immunol, 2022, 13:919444
|
|
| S8931 |
SB290157 trifluoroacetate
|
SB290157 trifluoroacetate (SB 290157 TFA) is a potent, competitive and selective antagonist of C3a receptor (C3aR) with IC50 of 200 nM for RBL-C3aR. |
-
CNS Neurosci Ther, 2025, 31(1):e70216
-
Invest Ophthalmol Vis Sci, 2025, 66(5):2
-
Cell Death Dis, 2023, 14(4):285
|
|
| S3612 |
Rosmarinic acid
|
Rosmarinic acid (RA, Rosemary acid) is a naturally occurring hydroxylated compound. It has the ability to block complement fixation, inhibit lipoxygenase and cyclooxygenase activity and inhibit the expression of CCL11 and CCR3 by suppressing the IKK-β activity in NF-κB activation signaling.
|
-
Theranostics, 2025, 15(6):2523-2543
-
World J Clin Oncol, 2025, 16(5):105341
-
Free Radic Biol Med, 2021, S0891-5849(21)00198-2
|
|
| S0525 |
ADH-503 (GB1275)
|
ADH-503 (GB1275, (Z)-Leukadherin-1 choline) is the salt form of leukadherin-1 and acts as a potent allosteric agonist of CD11b. |
-
Front Immunol, 2025, 16:1420325
|
|
| S3240 |
Phaseoloidin
|
Phaseoloidin, a homogentisic acid glucoside from Nicotiana attenuata trichomes, contributes to the plant's resistance against lepidopteran herbivores. Phaseoloidin has anti-complement effects. |
|
|
| E1048 |
JR14a
|
JR14a, a selective and potent human Complement C3a receptor antagonist, which is assessed by inhibition of intracellular calcium release (IC50=10 nM) induced in human monocyte-derived macrophages by C3a, inhibition of β-hexosaminidase secretion (IC50=8 nM) from human LAD2 mast cells degranulated by C3a, and selectivity for human C3aR over C5aR. |
|
|
| P1269New |
Pegcetacoplan acetate
|
Pegcetacoplan acetate, a PEGylated cyclic peptide, is the first approved inhibitor of complement component C3/C3b designed to treat adults with Paroxysmal Nocturnal Hemoglobinuria (PNH). It binds C3 and C3b to inhibit convertase-mediated C3 cleavage, blocking C3b opsonization (extravascular hemolysis) and downstream MAC formation (intravascular hemolysis). |
|
|
| S0803 |
Danicopan
|
Danicopan is a potent, selective and orally active inhibitor of factor D with Kd of 0.54 nM for human Factor D. Danicopan inhibits alternative pathway of complement (APC) activity, and has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS). |
|
|
| E0119 |
LNP023 (Iptacopan) Hydrochloride
|
Iptacopan (LNP023) Hydrochloride is a first-in-class, orally administered, potent and highly selective factor B inhibitor with an IC50 of 12 nM and a Kd value of 7.9 nM. Iptacopan exhibits excellent selectivity over other proteases affording IC50s of >30 μM across a panel of 41 human proteases. |
|
|
| S9138 |
Picfeltarraenin IA
|
Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system. |
|
|
| S8306 |
Leukadherin-1
|
Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)). |
-
International Immunopharmacology, 2023, Volume 118
-
Int Immunopharmacol, 2023, 118:110024
-
Front Immunol, 2022, 13:919444
|
|
| S0525 |
ADH-503 (GB1275)
|
ADH-503 (GB1275, (Z)-Leukadherin-1 choline) is the salt form of leukadherin-1 and acts as a potent allosteric agonist of CD11b. |
-
Front Immunol, 2025, 16:1420325
|
|
| S1322 |
Dexamethasone
|
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients. |
- Signal Transduct Target Ther, 2025, 10(1):230
- Signal Transduct Target Ther, 2025, 10(1):394
- Gut, 2025, gutjnl-2025-336105
|
|
| S2286 |
Cyclosporin A
|
Cyclosporin A, a non-polar cyclic oligopeptide, is an immunosuppressive agent that binds to cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay. Cyclosporin A is generally given following transplant surgery to prevent rejection and has been used to test its toxic effect on a perfused 3D proximal tubule model.Cyclosporin A (NSC 290193) can be used to induce animal models of Chronic Rejection of Liver Transplantation. |
- Signal Transduct Target Ther, 2025, 10(1):81
- Signal Transduct Target Ther, 2025, 10(1):167
- Adv Sci (Weinh), 2025, 12(36):e06150
|
|
| S3124 |
Dexamethasone Acetate
|
Dexamethasone (NSC 39471,Dexamethasone 21-acetate) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
- Acta Pharm Sin B, 2024, 14(8):3528-3542
- STAR Protoc, 2023, 4(2):102342
- Exp Mol Med, 2022, 54(9):1450-1460
|
|
| S4028 |
Dexamethasone Sodium Phosphate
|
Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. |
- Proc Natl Acad Sci U S A, 2025, 122(12):e2426107122
- J Tradit Chin Med, 2025, 45(4):739-746
- Cancer Cell, 2024, 42(9):1507-1527.e11
|
|
| S8522 |
Compstatin
|
Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. |
- Nat Commun, 2025, 16(1):2493
- Proc Natl Acad Sci U S A, 2025, 122(20):e2412447122
- CNS Neurosci Ther, 2025, 31(1):e70216
|
|
| S3612 |
Rosmarinic acid
|
Rosmarinic acid (RA, Rosemary acid) is a naturally occurring hydroxylated compound. It has the ability to block complement fixation, inhibit lipoxygenase and cyclooxygenase activity and inhibit the expression of CCL11 and CCR3 by suppressing the IKK-β activity in NF-κB activation signaling.
|
- Theranostics, 2025, 15(6):2523-2543
- World J Clin Oncol, 2025, 16(5):105341
- Free Radic Biol Med, 2021, S0891-5849(21)00198-2
|
|
| S3240 |
Phaseoloidin
|
Phaseoloidin, a homogentisic acid glucoside from Nicotiana attenuata trichomes, contributes to the plant's resistance against lepidopteran herbivores. Phaseoloidin has anti-complement effects. |
|
|
| P1269New |
Pegcetacoplan acetate
|
Pegcetacoplan acetate, a PEGylated cyclic peptide, is the first approved inhibitor of complement component C3/C3b designed to treat adults with Paroxysmal Nocturnal Hemoglobinuria (PNH). It binds C3 and C3b to inhibit convertase-mediated C3 cleavage, blocking C3b opsonization (extravascular hemolysis) and downstream MAC formation (intravascular hemolysis). |
|
|
| S0803 |
Danicopan
|
Danicopan is a potent, selective and orally active inhibitor of factor D with Kd of 0.54 nM for human Factor D. Danicopan inhibits alternative pathway of complement (APC) activity, and has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS). |
|
|
| E0119 |
LNP023 (Iptacopan) Hydrochloride
|
Iptacopan (LNP023) Hydrochloride is a first-in-class, orally administered, potent and highly selective factor B inhibitor with an IC50 of 12 nM and a Kd value of 7.9 nM. Iptacopan exhibits excellent selectivity over other proteases affording IC50s of >30 μM across a panel of 41 human proteases. |
|
|
| S9138 |
Picfeltarraenin IA
|
Picfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system. |
|
|