TRAM-34

TRAM-34 : Inhibitor of KCNN4

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe TRAM-34 is in the process of SERP review.

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Information

KCNN4

Inhibitor

up to 5 uM
Reviewer recommended concentration: up to 200 nM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): TRAM-34 was screened against a panel of 15 other channels. TRAM-34 is 200- to 1,500-fold less effective against several related mammalian potassium channels: Kv1.1-Kv1.5, Kv3.1, Kv4.2, Kir2.1, BKCa, including the closely related cloned SKCa channels (rSKCa2, hSKCa2, hSKCa3) as well as the native SKCa in Jurkat T cells. The CRAC calcium channel, the human SKMI-sodium channel, the swelling-activated chloride channel in activated human T lymphocytes, and the native chloride channel in COS-7 cells are also insensitive to TRAM-34

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Results should be interpreted with caution and reference made to reported off-target activities against nonselective cation channels (doi: 10.1007/s00424-007-0232-4), several rodent and human cytochrome P450 enzymes (doi: 10.1371/journal.pone.0063028)

(last updated: 7 Dec 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

TRAM-34 has been commercialized a blocker of KCa3.1for many years, considering vast family of channel and transporter proteins vs medium molecular size of TRAM-34, a thorough test of TRAM-34 against majority candidate protein is still challenging, recommend to use it at dose below 200nM

(last updated: 7 Dec 2022 )