A membrane-permeable blocker of IKCa1/KCa3.1 (Kds = 20 and 25 nM for the cloned and native channel in COS-7 cells and human T lymphocytes

TRAM-34 – 5 mg

Brand:
Cayman
CAS:
289905-88-0
Storage:
-20
UN-No:
Non-Hazardous - /

TRAM-34 is a membrane-permeable inhibitor of the intermediate-conductance calcium-activated potassium channel (IKCa1/KCa3.1).{41340} It blocks IKCa1 (Kds = 20 and 25 nM for the cloned and native channel in COS-7 cells and human T lymphocytes, respectively) with 200- to 1,500-fold selectivity for IKCa1 over Kv (Kv1.1-Kv1.5, Kv3.1, Kv4.2), Kir2.1, BKCa (Slo), SKCa (rSKCa2, hSKCa2, hSKCa3), native SKCa, and CRAC in Jurkat T cells, as well as sodium and chloride channels. It also inhibits nonselective lysophosphatidylcholine-induced cation currents (IC50 = 38 nM).{41342} TRAM-34 suppresses reactivation of human-derived T lymphocytes stimulated with anti-CD3 antibody after an initial pretreatment to upregulate IKCa1 channels (mean EC50s = 295 and 910 nM from sensitive and less sensitive human donors, respectively).{41340} It does not reduce viability of human T lymphocytes at a concentration of 5 μM over 48 hours incubation. In vitro, TRAM-34 (10-40 μM) inhibits proliferation of human endometrial cancer cells and induces cell cycle arrest at the G0/G1 phase.{41343} It also inhibits proliferation of LNCaP and PC3 prostate cancer cells and proliferation induced by epidermal growth factor (EGF) in smooth muscle A7r5 cells (IC50 = 8 nM).{41344,41341} In vivo, TRAM-34 (120 mg/kg per day) reduces intimal hyperplasia by approximately 40% after 1, 2, and 6 weeks in a rat model of balloon catheter injury. TRAM-34 (30 μM) treatment of HEC-1-A cells prior to flank implantation into nude mice slows tumor growth in vivo.  

 

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Description

A membrane-permeable blocker of IKCa1/KCa3.1 (Kds = 20 and 25 nM for the cloned and native channel in COS-7 cells and human T lymphocytes, respectively); 200- to 1,500-fold selective for IKCa1 over Kv (Kv1.1-Kv1.5, Kv3.1, Kv4.2), Kir2.1, BKCa (Slo), SKCa (rSKCa2, hSKCa2, hSKCa3), native SKCa, and CRAC in Jurkat T cells as well as sodium and chloride channels; suppresses reactivation of human-derived T lymphocytes stimulated with anti-CD3 antibody (mean EC50s = 295 and 910 nM from sensitive and less sensitive human donors, respectively); inhibits proliferation of human endometrial cancer cells and induces cell cycle arrest at the G0/G1 phase; inhibits proliferation of LNCaP and PC3 prostate cancer cells; inhibits proliferation induced by epidermal growth factor (EGF) in smooth muscle A7r5 cells (IC50 = 8 nM); reduces intimal hyperplasia by approximately 40% after 1, 2, and 6 weeks in a rat model of balloon catheter injury when administered at a dose of 120 mg/kg per day; pretreatment of HEC-1-A cells with TRAM-34 at a concentration of 30 μM inhibits tumor growth in vivo in nude mice

Formal name: 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole

Synonyms: 

Molecular weight: 344.8

CAS: 289905-88-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Immunology & Inflammation|Adaptive Immunity

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