TANZISERTIB

TANZISERTIB : Inhibitor of JNK1, JNK2, JNK3

Structure

SERP Rating

In Cells

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In Model Organisms

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Information

MAPK8
MAPK9
MAPK10

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P45983

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 61 ± 24 nM

Potency Assay: Biochemical assay

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

Target aliases:

Mitogen-activated protein kinase 8, SAPK1C, SAPK1, ...

DOI Reference: 10.1016/j.bmcl.2011.12.027

Uniprot ID: P45983

Target Class: Kinase

Target SubClass: CMGC

Potency: Ki

Potency Value: 44 ± 3 nM

Potency Assay: Competitive binding assay

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

Target aliases:

Mitogen-activated protein kinase 8, SAPK1C, SAPK1, ...

DOI Reference: 10.1016/j.bmcl.2011.12.027

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selective against MAP kinases ERK1 and p38α with IC50 of 0.48 and 3.4 μM respectively.

Potency assay (off target): Tanzisertib showed remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kinase inhibited more than 50% at 3 μM (IC50 = 0.38 μM). It inhibited no receptor at greater than 50% at 10 μM concentration in a panel of 75 receptors, ion channels and neurotransmitter transporters. Finally, when tested against 22 diverse non-kinase enzymes at 10 μM, no inhibition greater than 50% was observed.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Tanzisertib is a high-quality chemical probe for potently inhibiting JNK1, JNK2, and JNK3. It is > 20-fold selective over p38 and ERK1, although it does have modest off-target activity (IC50 ~ 400 nM) against GAK, EGFR, and some other MAP kinases (specific ones not disclosed in Krenitsky et al.). For cellular studies, 1 uM is a suitable dose, and practitioners should be aware that significant EGFR inhibition will occur at doses > 3 uM. Tanzisertib is orally bioavailable in all pre-clinical species and has demonstrated efficacy in acute LPS-induced TNFa and chronic bleomycin-induced pulmonary fibrosis rat models at doses 30-50 mg/kg.

(last updated: 21 May 2025 )