TRAM-34   Click here for help

GtoPdb Ligand ID: 2336

Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: TRAM-34 is a KCa3.1 channel blocker.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 1
Hydrogen bond donors 0
Rotatable bonds 4
Topological polar surface area 17.82
Molecular weight 344.11
XLogP 6.47
No. Lipinski's rules broken 1
Click here for help
Canonical SMILES Clc1ccccc1C(n1cccn1)(c1ccccc1)c1ccccc1
Isomeric SMILES Clc1ccccc1C(n1cccn1)(c1ccccc1)c1ccccc1
InChI InChI=1S/C22H17ClN2/c23-21-15-8-7-14-20(21)22(25-17-9-16-24-25,18-10-3-1-4-11-18)19-12-5-2-6-13-19/h1-17H
1. Chen YJ, Lam J, Gregory CR, Schrepfer S, Wulff H. (2013)
The Ca²⁺-activated K⁺ channel KCa3.1 as a potential new target for the prevention of allograft vasculopathy.
PLoS ONE, 8 (11): e81006. [PMID:24312257]
2. Chen YJ, Nguyen HM, Maezawa I, Grössinger EM, Garing AL, Köhler R, Jin LW, Wulff H. (2016)
The potassium channel KCa3.1 constitutes a pharmacological target for neuroinflammation associated with ischemia/reperfusion stroke.
J Cereb Blood Flow Metab, 36 (12): 2146-2161. [PMID:26661208]
3. Chimote AA, Hajdu P, Kucher V, Boiko N, Kuras Z, Szilagyi O, Yun YH, Conforti L. (2013)
Selective inhibition of KCa3.1 channels mediates adenosine regulation of the motility of human T cells.
J Immunol, 191 (12): 6273-80. [PMID:24227782]
4. Crottès D, Félix R, Meley D, Chadet S, Herr F, Audiger C, Soriani O, Vandier C, Roger S, Angoulvant D et al.. (2016)
Immature human dendritic cells enhance their migration through KCa3.1 channel activation.
Cell Calcium, 59 (4): 198-207. [PMID:27020659]
5. Friebel K, Schönherr R, Kinne RW, Kunisch E. (2015)
Functional role of the KCa3.1 potassium channel in synovial fibroblasts from rheumatoid arthritis patients.
J Cell Physiol, 230 (7): 1677-88. [PMID:25545021]
6. Glaser N, Little C, Lo W, Cohen M, Tancredi D, Wulff H, O'Donnell M. (2017)
Treatment with the KCa3.1 inhibitor TRAM-34 during diabetic ketoacidosis reduces inflammatory changes in the brain.
Pediatr Diabetes, 18 (5): 356-366. [PMID:27174668]
7. Hua X, Deuse T, Chen YJ, Wulff H, Stubbendorff M, Köhler R, Miura H, Länger F, Reichenspurner H, Robbins RC et al.. (2013)
The potassium channel KCa3.1 as new therapeutic target for the prevention of obliterative airway disease.
Transplantation, 95 (2): 285-92. [PMID:23325003]
8. Koshy S, Wu D, Hu X, Tajhya RB, Huq R, Khan FS, Pennington MW, Wulff H, Yotnda P, Beeton C. (2013)
Blocking KCa3.1 channels increases tumor cell killing by a subpopulation of human natural killer lymphocytes.
PLoS ONE, 8 (10): e76740. [PMID:24146918]
9. Köhler R, Wulff H, Eichler I, Kneifel M, Neumann D, Knorr A, Grgic I, Kämpfe D, Si H, Wibawa J, Real R, Borner K, Brakemeier S, Orzechowski HD, Reusch HP, Paul M, Chandy KG, Hoyer J. (2003)
Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis.
Circulation, 108 (9): 1119-25. [PMID:12939222]
10. Lin H, Zheng C, Li J, Yang C, Hu L. (2014)
Ca2+ -activated K+ channel-3.1 blocker TRAM-34 alleviates murine allergic rhinitis.
Int Immunopharmacol, 23 (2): 642-8. [PMID:25466273]
11. Ohya S, Fukuyo Y, Kito H, Shibaoka R, Matsui M, Niguma H, Maeda Y, Yamamura H, Fujii M, Kimura K et al.. (2014)
Upregulation of KCa3.1 K(+) channel in mesenteric lymph node CD4(+) T lymphocytes from a mouse model of dextran sodium sulfate-induced inflammatory bowel disease.
Am J Physiol Gastrointest Liver Physiol, 306 (10): G873-85. [PMID:24674776]
12. Roach KM, Duffy SM, Coward W, Feghali-Bostwick C, Wulff H, Bradding P. (2013)
The K+ channel KCa3.1 as a novel target for idiopathic pulmonary fibrosis.
PLoS ONE, 8 (12): e85244. [PMID:24392001]
13. Shao Z, Gaurav R, Agrawal DK. (2015)
Intermediate-conductance calcium-activated potassium channel KCa3.1 and chloride channel modulate chemokine ligand (CCL19/CCL21)-induced migration of dendritic cells.
Transl Res, 166 (1): 89-102. [PMID:25583444]
14. Wulff H, Miller MJ, Hansel W, Grissmer S, Cahalan MD, Chandy KG. (2000)
Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant.
Proc Natl Acad Sci USA, 97 (14): 8151-6. [PMID:10884437]
15. Yu ZH, Xu JR, Wang YX, Xu GN, Xu ZP, Yang K, Wu DZ, Cui YY, Chen HZ. (2013)
Targeted inhibition of KCa3.1 channel attenuates airway inflammation and remodeling in allergic asthma.
Am J Respir Cell Mol Biol, 48 (6): 685-93. [PMID:23492185]
16. Zhang S, Wang X, Ju C, Zhu L, Du Y, Gao C. (2016)
Blockage of K(Ca)3.1 and Kv1.3 channels of the B lymphocyte decreases the inflammatory monocyte chemotaxis.
Int Immunopharmacol, 31: 266-71. [PMID:26795234]