SGC-CK2-2

SGC-CK2-2 : Inhibitor of CSNK2A1, CSNK2A2

Structure

SERP Rating

In Cells

(2 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.

Probe SGC-CK2-2 is in the process of SERP review.

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Information

CSNK2A1
CSNK2A2

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P68400

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: IC50

Potency Value: 3.0 nM

Potency Assay: DiscoverX assay

PDB ID for probe-target interaction (3D structure): 8BGC

Target aliases:

Casein kinase II subunit alpha, CK2A1, CSNK2A1, CS ...

DOI Reference: 10.1021/acsmedchemlett.2c00530

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): SGC-CK2-2 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM. Only 3 kinases showed PoC <10 giving an S10(1 μM) = 0.007. When the PoC <35 fraction was examined, 13 kinases were included (S35(1 μM) = 0.032). The closest off-target kinase based on enzymatic potency is HIPK2 (IC50 = 600 nM, 200-fold selectivity window).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Given the lack of proteome-wide profiling, unknown non-kinase targets cannot be excluded.

(last updated: 9 Jun 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Not recommended for cellular work since this compound showed poor activity for inhibiting AKT phosphorylation. NanoBRET showed inconsistent IC50 with enzymatic assay.

(last updated: 17 Jun 2024 )