SGC-CAMKK2-1

SGC-CAMKK2-1 : Inhibitor of CAMKK1, CAMKK2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

CAMKK1
CAMKK2

Inhibitor

up to 5 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q8N5S9

Target Class: Kinase

Target SubClass: Other STK

Potency: Activity

Potency Value: 12 Percent of Control

Potency Assay: KINOMEscan assay at 1 µM

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Calcium/calmodulin-dependent protein kinase kinase ...

DOI Reference: 10.3390/cells12020287

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

SGC-CAMKK2-1 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 uM. Only two kinases demonstrated percentage of control (PoC) values of less than 15% (CAMKK2 PoC = 5.4, CAMKK1 PoC = 12), indicating excellent kinome wide selectivity.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This exact compound is not detailed in the reference. The detailed compound is the phenyl ring on the 5-position of the azabenzofuran system. This particular compound has the 3-methylphenyl. More detailed work is needed prior to fully recommending its usage.

(last updated: 22 Apr 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

The kinome selectivity profile of this probe is exceptional. The inactive analogue is also of high quality and it is well worth using in parallel with the probe to obtain conclusive results. The lipophilic nature of this probe coupled with the carboxylic acid head group make it highly likely to exhibit binding to serum albumin. The presence and percentage of serum in cellular media might influence cellular potency by the probe as a result. There are no peer reviewed references as of April 2022 but a graduate thesis documenting its use in oncology investigations is listed online and may provide helpful information to users: "CAMKK2 PROMOTES PROSTATE CANCER PROGRESSION THROUGH INDEPENDENT INTRINSIC AND EXTRINSIC ROLES" by Thomas Lloyd Pulliam (https://hdl.handle.net/10657/8271). There is no evidence as of the time of this review about the feasibility of using this probe in vivo.

(last updated: 22 Apr 2022 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a potent and selective compound for CAMKK2 . However, the cellular potency is slightly above the suggested 1 µM threshold and effect of the compound on cellular viability would have been nice to report.

(last updated: 23 May 2024 )