Cat. No.: HY-139896

Odemsertib

Name: Odemsertib
Brand: MedChemExpress
SKU: HY-139896
Availability: PreOrder

(Synonyms: R835)

Odemsertib (R835) is a selective, orally active IRAK1/IRAK4 inhibitor with IC₅₀ values of 15 nM and 14 nM, respectively. Odemsertib blocks TLR/IL-1R/MyD88 signaling, IRAK4 autophosphorylation, NF-κB/MAPK activation, and pro-inflammatory cytokine production. Odemsertib does not inhibit TBK1- or TNFR-driven NF-κB/MAPK activation and shows minimal inhibition of TLR3/TRIF-dependent cytokine release. Odemsertib can be used for research on inflammatory and autoimmune diseases.

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

CAS No.: 2033070-96-9
Formula: C₂₃H₂₃F₂N₇O₂S
Molecular Weight:499.54

Storage:

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

Odemsertib Chemical Structure

CAS No.: 2033070-96-9

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[3]

IRAK1

15 nM (IC₅₀)

IRAK4

14 nM (IC₅₀)

All IRAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
NHDF	IC50	>16 nM	Estimated IC50 greater than 16 nM for inhibition of IL-1β-induced phospho-IRAK4 in normal human dermal fibroblasts by Western blotting. Estimated IC50 greater than 16 nM for inhibition of IL-1β-induced phospho-IRAK4 in normal human dermal fibroblasts by Western blotting.	s41598-026-62719-5
NHDF	IC50	0.016 μM	Estimated inhibition of IL-1β-induced downstream phospho-IKK, phospho-NF-κB, phospho-p38, and phospho-JNK in normal human dermal fibroblasts by Western blotting. Estimated inhibition of IL-1β-induced downstream phospho-IKK, phospho-NF-κB, phospho-p38, and phospho-JNK in normal human dermal fibroblasts by Western blotting.	s41598-026-62719-5
THP-1	EC50	0.081 μM	Inhibition of TLR4/LPS-induced IL-23 production in THP-1 human monocytic cells assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced IL-23 production in THP-1 human monocytic cells assessed by ELISA/Luminex.	s41598-026-62719-5
THP-1	IC50	81 nM	Inhibition of TLR4/LPS-induced IL-23 production in THP-1 human monocytic cells assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced IL-23 production in THP-1 human monocytic cells assessed by ELISA/Luminex.	s41598-026-62719-5
THP-1	EC50	0.127 μM	Inhibition of TLR4/LPS-induced TNF-α production in THP-1 human monocytic cells assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced TNF-α production in THP-1 human monocytic cells assessed by ELISA/Luminex.	s41598-026-62719-5
Dendritic cell	EC50	0.380 μM	Inhibition of TLR4/LPS-induced IL-23 production in human dendritic cells assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced IL-23 production in human dendritic cells assessed by ELISA/Luminex.	s41598-026-62719-5
Dendritic cell	EC50	0.039 μM	Inhibition of TLR7/Gardiquimod-induced IFN-α production in human dendritic cells assessed by ELISA/Luminex. Inhibition of TLR7/Gardiquimod-induced IFN-α production in human dendritic cells assessed by ELISA/Luminex.	s41598-026-62719-5
Dendritic cell	EC50	0.137 μM	Inhibition of TLR2/LTA-induced IL-6 production in human dendritic cells assessed by ELISA/Luminex. Inhibition of TLR2/LTA-induced IL-6 production in human dendritic cells assessed by ELISA/Luminex.	s41598-026-62719-5
Macrophage	EC50	0.042 μM	Inhibition of TLR4/LPS-induced IL-6 production in human macrophages assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced IL-6 production in human macrophages assessed by ELISA/Luminex.	s41598-026-62719-5
Macrophage	EC50	0.038 μM	Inhibition of TLR4/LPS-induced TNF-α production in human macrophages assessed by ELISA/Luminex. Inhibition of TLR4/LPS-induced TNF-α production in human macrophages assessed by ELISA/Luminex.	s41598-026-62719-5
HUVEC	EC50	0.051 μM	Inhibition of IL-1R/IL-1β-induced IL-6 production in HUVEC assessed by ELISA/Luminex. Inhibition of IL-1R/IL-1β-induced IL-6 production in HUVEC assessed by ELISA/Luminex.	s41598-026-62719-5
HUVEC	IC50	51 nM	Inhibition of IL-1R/IL-1β-induced IL-6 production in HUVEC assessed by ELISA/Luminex. Inhibition of IL-1R/IL-1β-induced IL-6 production in HUVEC assessed by ELISA/Luminex.	s41598-026-62719-5
NHDF	EC50	0.049 μM	Inhibition of IL-1R/IL-1β-induced G-CSF production in normal human dermal fibroblasts assessed by ELISA/Luminex. Inhibition of IL-1R/IL-1β-induced G-CSF production in normal human dermal fibroblasts assessed by ELISA/Luminex.	s41598-026-62719-5
NHDF	EC50	0.036 μM	Inhibition of IL-1R/IL-1β-induced GM-CSF production in normal human dermal fibroblasts assessed by ELISA/Luminex. Inhibition of IL-1R/IL-1β-induced GM-CSF production in normal human dermal fibroblasts assessed by ELISA/Luminex.	s41598-026-62719-5
THP-1	EC50	0.092 μM	Inhibition of TLR4/nigericin-induced pyroptosis in LPS-primed THP-1 human monocytic cells assessed by CellTiter-Glo. Inhibition of TLR4/nigericin-induced pyroptosis in LPS-primed THP-1 human monocytic cells assessed by CellTiter-Glo.	s41598-026-62719-5
THP-1	EC50	0.139 μM	Inhibition of TLR4/nigericin-induced pyroptosis in LPS-primed THP-1 human monocytic cells assessed by LDH release. Inhibition of TLR4/nigericin-induced pyroptosis in LPS-primed THP-1 human monocytic cells assessed by LDH release.	s41598-026-62719-5
THP-1	EC50	0.100 μM	Inhibition of TLR4/nigericin-induced active caspase-1 release in LPS-primed THP-1 human monocytic cells. Inhibition of TLR4/nigericin-induced active caspase-1 release in LPS-primed THP-1 human monocytic cells.	s41598-026-62719-5
THP-1	EC50	0.014 μM	Inhibition of TLR4/nigericin-induced IL-1β production in LPS-primed THP-1 human monocytic cells. Inhibition of TLR4/nigericin-induced IL-1β production in LPS-primed THP-1 human monocytic cells.	s41598-026-62719-5
THP-1	EC50	0.134 μM	Inhibition of TLR4/nigericin-induced S100A8/A9 release in LPS-primed THP-1 human monocytic cells. Inhibition of TLR4/nigericin-induced S100A8/A9 release in LPS-primed THP-1 human monocytic cells.	s41598-026-62719-5

In Vitro

Innate ImmunityCytokines & ChemokinesInflammasomePyroptosisOthers

Innate Immunity

Odemsertib (R835) (250 nM-1 µM) is an equipotent biochemical inhibitor of IRAK1 and IRAK4 (IC₅₀ 0.015 and 0.014 µM, respectively) and shows selectivity in a 97-kinase panel^[3].

Innate Immunity

Cytokines & Chemokines

Odemsertib (0.64 nM-10 µM; 15-30 min IL-1β; 3 h LPS) selectively inhibits IRAK4 autophosphorylation, IRAK1 degradation, and IRAK-dependent NF-κB/MAPK signaling in NHDF and THP-1 cells, with an estimated downstream IC₅₀ of ~0.016 µM, without inhibiting TBK1 or TNF-α-driven signaling^[3].
Odemsertib potently inhibits TLR- and IL-1R-dependent cytokine production across human immune and stromal cells, with EC₅₀ values ranging from 0.036 to 0.380 µM^[3].

Innate Immunity

Cytokines & Chemokines

Inflammasome

Pyroptosis

Odemsertib blocks TLR4/Nigericin (HY-127019)-dependent NLRP3 inflammasome priming/activation and pyroptosis in THP-1 cells, with an IL-1β EC₅₀ of 0.014 µM^[3].

Others

Odemsertib retains cell-based selectivity for IRAK1/IRAK4 over TAK1, HGK, LRRK2, and Flt3, with HGK EC₅₀ >10 µM^[3].

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

Parmacokinetics

Species	Dose	Route	Plasma Concentration
Mice^[3]	15 mg/kg	p.o.	1127 ng/mL

In Vivo

Innate ImmunityCytokines & ChemokinesInflammasome

Innate Immunity

Cytokines & Chemokines

Odemsertib (R835) (1-45 mg/kg; oral gavage; single pretreatment 30 minutes before IL-1β challenge) dose-dependently inhibits IL-1β-induced serum IL-6 production in mice^[3].
Odemsertib (1-45 mg/kg; oral gavage; single pretreatment 30 minutes before LPS challenge) dose-dependently suppresses LPS-induced serum cytokines in mice^[3].

Innate Immunity

Cytokines & Chemokines

Inflammasome

Odemsertib (5-45 mg/kg; oral gavage; single pretreatment 30 minutes before MSU challenge) dose-dependently reduces MSU-induced serum and peritoneal inflammatory cytokines and peritoneal neutrophil recruitment in mice, while serum IL-1β remains unchanged^[3].

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

Animal Model:

BALB/c (female; approximately 11 weeks old; 16-21 g)^[3]
Dosage:

1, 2, 5, 15, and 45 mg/kg
Administration:

oral gavage; single pretreatment 30 minutes before IL-1β challenge
Result:

In the higher-dose study, serum IL-6 was reduced by 86%, 85%, and 93% at 5, 15, and 45 mg/kg, respectively, compared with vehicle.
In the lower-dose study, mean serum IL-6 was reduced by 32%, 46%, and 64% at 1, 2, and 5 mg/kg, respectively, compared with vehicle.
The ED50 corresponded to approximately 2 mg/kg.

Animal Model:

BALB/c (female; 9 weeks old; 17-21 g)^[3]
Dosage:

5, 15, and 45 mg/kg
Administration:

oral gavage; single pretreatment 30 minutes before MSU challenge
Result:

Dose-dependent reductions in serum IL-6, KC, and G-CSF were observed compared with vehicle; peritoneal cytokine levels mirrored the serum results.
MSU challenge increased serum IL-6, KC, and G-CSF versus naive mice, while serum IL-1β remained unchanged.
Peritoneal neutrophil numbers were 0.7 × 10^6, 0.6 × 10^6, and 0.4 × 10^6 at 5, 15, and 45 mg/kg, respectively, compared with 1.0 × 10^6 in vehicle controls.

Animal Model:

BALB/c (female; 9 weeks old; 17-21 g)^[3]
Dosage:

1, 2, 5, 15, and 45 mg/kg
Administration:

oral gavage; single pretreatment 30 minutes before LPS challenge
Result:

Significant dose-dependent reductions in serum TNF, MIP-2, KC, IL-23, MCP-1, IL-6, and G-CSF levels occurred at 3 hours post-challenge compared with vehicle-treated animals.
At the 15 mg/kg dose level (plasma concentration 1127 ng/mL), serum IL-6, TNF-α, and KC were reduced by 88%, 99%, and 81%, respectively.

Related Protocols :

Research Protocol for Inflammation-related Diseases

Chemical Information

CAS No. 2033070-96-9
Molecular Weight 499.54
Formula C₂₃H₂₃F₂N₇O₂S
SMILES

O=C(C1=CSC(C2=CNN=C2)=N1)NC3=CN([C@]4([H])CC[C@H](CC4)OCC)N=C3C5=C(C=CC(F)=N5)F
Synonyms

R835
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]. L. Yan, et al. THU0219 FIRST-INHUMAN STUDY OF SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS OF IRAK1/4 INHIBITOR R835 IN HEALTHY SUBJECTS. Annals of the Rheumatic Diseases, June 2020

[2]. C. Lamagna, et al. FRI0016 R835, A NOVEL IRAK1/4 DUAL INHIBITOR IN CLINICAL DEVELOPMENT, BLOCKS TOLL-LIKE RECEPTOR 4 (TLR4) SIGNALING IN HUMAN AND MOUSE. Annals of the Rheumatic Diseases, June 2020.

[3]. Shaw, S.J., et al. Preclinical characterization and early development of R835, a novel, selective dual IRAK1 and IRAK4 inhibitor. Sci Rep (2026).

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Odemsertib

All IRAK Isoforms