YYSW001

YYSW001 : Inhibitor of JAK1

Structure

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Probe YYSW001 is in the process of SERP review.

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Information

JAK1

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P23458

Target Class: Kinase

Target SubClass: Tyr kinase

Potency: IC50

Potency Value: 6 ± 0.3 nM

Potency Assay: Biochemical Assay

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

Target aliases:

Tyrosine-protein kinase JAK1, JAK1B, JAK1A, JAK1, ...

DOI Reference: 10.1021/acs.jmedchem.5c03183

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KinomeSCAN Screening at concentration of 1000 nM, against a panel of 403 kinases demonstrated remarkable specificity.

Probe Selectivity in Vitro:

YYSW001 potently inhibited only two kinases, which were the intended target JAK1 and the only off-target DCLK3, whose expression is restricted to the brain. It exhibited less pronounced inhibition against a further 14 kinases, including the other JAK family members, while the remaining kinome was largely unaffected. JAK2: IC50 for JAK2, JAK3, and TYK2 IC50 > 300 nM

Potency assay, off target (cells): GM-CSF-induced STAT5 phosphorylation (JAK2-STAT5 IC50 = 5.530 μM).

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