TRAM-34 289905-88-0

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Molecular Weight:

344.84 TRAM-34 is a selective and Potent Inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450.

Biological Activity

Unlike clotrimazole, TRAM-34 selectively inhibits IKCa1 without blocking
cytochrome P450 enzyme (CYP3A4). TRAM-34 potently inhibits cloned IKCa1
channel in IKCa1-transfected COS-7 cells as well as native IKCa
currents in human T lymphocytes and T84 cells with Kd of 20
nM, 25 nM, and 22 nM, respectively, more potently than clotrimazole with
Kd of 70 nM, 100 nM, and 90 nM, respectively.


TRAM-34 exhibits 200- to
1,500-fold selectivity over Other ion channels such as KV, BKCa, SKCa,
Na+, CRAC and Cl- channels. TRAM-34 significantly
inhibits anti-CD3 Ab or PKC-activator PMA plus calcium-ionophore
ionomycin induced activation of human T lymphocytes with IC50 of 295-910
nM and 85-830 nM, respectively. TRAM-34 (5 μM) does not inhibit cell
viability of human T lymphocytes or several cell lines.


TRAM-34 significantly inhibits EGF-induced IKCa1 up-regulation, and
EGF-stimulated proliferation of A7r5 cells with IC50 of 8 nM. TRAM-34 treatment inhibits proliferation of human endometrial cancer (EC) cells, and blocks EC Cell Cycle at G0/G1 phase. Inhibition of the IKCa1 channel by TRAM-34 (1-30 μM) leads to
dose-dependent suppression of the proliferation but not Apoptosis of
LNCaP and PC-3 prostate cancer (PCa) cells, involving an increase of
p21Cip1 and cell arrest in the G1 cycle.


TRAM-34 treatment at ~500-1,000 times the channel-blocking dose (0.5 mg/kg/day) for 7 days is nontoxic to mice. Administration of TRAM-34 at 120 mg/kg/day significantly reduces
intimal hyperplasia by ~40% in a rat model of balloon catheter injury
(BCI). Consistent with its in vitro role in inhibiting
the proliferation of EC cells, TRAM-34 treatment at 30 μM slows the
development of HEC-1-A tumor in vivo.

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Product Categories : Transmembrane Transporters > Potassium Channel Inhibitor