oJak-989

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oJak-989 is a selective JAK1 inhibitor with a K_i of 2.8 nM for JAK1, 110 nM for JAK3, and 31 nM for TYK2. oJak-989 is applicable to the research of inflammatory diseases.

For research use only. We do not sell to patients.

oJak-989 Chemical Structure

CAS No. : 1315485-91-6

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Purity & Documentation
References
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Description

oJak-989 is a selective JAK1 inhibitor with a K_i of 2.8 nM for JAK1, 110 nM for JAK3, and 31 nM for TYK2. oJak-989 is applicable to the research of inflammatory diseases^[1].

IC₅₀ & Target^[1]

JAK1

2.8 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>100 μM Compound: 21	Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay	[PMID: 23659214]
HEK293	IC₅₀	100 μM Compound: 21	Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay	[PMID: 23659214]
TF-1	EC₅₀	110 nM Compound: 21	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins	[PMID: 23659214]
TF-1	EC₅₀	180 nM Compound: 21	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood	[PMID: 23659214]

In Vitro

oJak-989 (Compound 21) is a potent and highly JAK1-selective inhibitor with a JAK1 K_i of 2.8 nM. It exhibits 26-fold selectivity over JAK2 in biochemical assays and 51-fold selectivity in cellular assays. Additionally, it possesses favorable MDCK permeability, low whole blood potency shift, high water solubility, and shows no significant hERG or clinically relevant CYP inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

286.34

Formula

C₁₅H₁₈N₄O₂

CAS No.

1315485-91-6

SMILES

[C@H](C)(O)C=1N(C2=C3C(NC=C2N1)=NC=C3)[C@H]4CCCOC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zak M, et al. Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2. J Med Chem. 2013;56(11):4764-4785. [Content Brief]

oJak-989 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

oJak-9891315485-91-6oJak989oJak 989JAKJanus kinaseJAK1IL-6JAK3JAK2TYK2pSTAT3pSTAT4IL-12E966D939Inhibitorinhibitorinhibit

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