IRAK4-IN-21

Name: IRAK4-IN-21
Brand: MedChemExpress
SKU: HY-151363
Rating: 4.5 (1 reviews)

Cat. No.: HY-151363 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC₅₀ values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC₅₀=0.17 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.

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

IRAK4-IN-21 Chemical Structure

CAS No. : 2170694-04-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 542	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 542	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 192	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
Dendritic cell	IC₅₀	0.51 μM Compound: 17	Antiinflammatory activity against human monocyte derived dendritic cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method Antiinflammatory activity against human monocyte derived dendritic cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method	[PMID: 35450353]
HUVEC	IC₅₀	0.18 μM Compound: 17	Antiinflammatory activity against HUVEC cells assessed as inhibition of LPS induced IL-6 production measured by ELISA method Antiinflammatory activity against HUVEC cells assessed as inhibition of LPS induced IL-6 production measured by ELISA method	[PMID: 35450353]
HUVEC	IC₅₀	0.2 μM Compound: 17	Antiinflammatory activity against HUVEC cells assessed as inhibition of IL-1beta induced IL-6 production preincubated with compound for 1 hr followed by IL-1beta stimulation and measured after 12 hrs by cell based ELISA method Antiinflammatory activity against HUVEC cells assessed as inhibition of IL-1beta induced IL-6 production preincubated with compound for 1 hr followed by IL-1beta stimulation and measured after 12 hrs by cell based ELISA method	[PMID: 35450353]
THP-1	IC₅₀	0.17 μM Compound: 17	Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS induced IL-23 production preincubated with compound for 1 hr followed by LPS stimulation and measured after 18 hrs by cell based ELISA method	[PMID: 35450353]

In Vitro

IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)^[1].

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

Cell Viability Assay^[1]

Cell Line:	THP-1, DC cells (are primed with IFN-γ)
Concentration:	10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time:	1 h (pre-incubate)
Result:	Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC₅₀ of 0.17 and 0.51 µM, respectively.

Cell Viability Assay^[1]

Cell Line:	HUVEC cells (IL-1β-stimulated)
Concentration:	10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time:	1 h (pre-incubate)
Result:	Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC₅₀ of 0.20 µM.

Cell Viability Assay^[1]

Cell Line:	Human whole blood (IL-1β-stimulated)
Concentration:	10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time:	1 h (pre-incubate)
Result:	Inhibited the level of MIP-1β in the human whole blood with an IC₅₀ of 0.47 µM.

In Vivo

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production^[1].

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

Animal Model:	BALB/c mice (acute mouse model; IL-1β-stimulated)^[1].
Dosage:	75 mg/kg
Administration:	Oral administration; single (pre-treat).
Result:	Showed 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h.

Molecular Weight

513.57

Formula

C₂₈H₂₈FN₇O₂

CAS No.

2170694-04-7

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@@H](C2)C=C[C@@H]2[C@H]1NC3=NC(NC4=CC=CC(C(N5CCCC5)=O)=C4)=NC=C3C6=CC(F)=CN=C6)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (194.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9472 mL	9.7358 mL	19.4715 mL
5 mM	0.3894 mL	1.9472 mL	3.8943 mL
10 mM	0.1947 mL	0.9736 mL	1.9472 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (251 KB) HNMR (187 KB) RP-HPLC (244 KB) LCMS (239 KB)

Handling Instructions (2659 KB)

References

[1]. Chen Y, et al. Discovery of 5-Aryl-2,4-diaminopyrimidine Compounds as Potent and Selective IRAK4 Inhibitors. ACS Med Chem Lett. 2022 Apr 4;13(4):714-719. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9472 mL	9.7358 mL	19.4715 mL	48.6789 mL
	5 mM	0.3894 mL	1.9472 mL	3.8943 mL	9.7358 mL
	10 mM	0.1947 mL	0.9736 mL	1.9472 mL	4.8679 mL
	15 mM	0.1298 mL	0.6491 mL	1.2981 mL	3.2453 mL
	20 mM	0.0974 mL	0.4868 mL	0.9736 mL	2.4339 mL
	25 mM	0.0779 mL	0.3894 mL	0.7789 mL	1.9472 mL
	30 mM	0.0649 mL	0.3245 mL	0.6491 mL	1.6226 mL
	40 mM	0.0487 mL	0.2434 mL	0.4868 mL	1.2170 mL
	50 mM	0.0389 mL	0.1947 mL	0.3894 mL	0.9736 mL
	60 mM	0.0325 mL	0.1623 mL	0.3245 mL	0.8113 mL
	80 mM	0.0243 mL	0.1217 mL	0.2434 mL	0.6085 mL
	100 mM	0.0195 mL	0.0974 mL	0.1947 mL	0.4868 mL

IRAK4-IN-21 Related Classifications

Inflammation/Immunology

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:

IRAK4-IN-212170694-04-7IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseplaque psoriasispsoriatic arthritisTHP-1DCHUVECInhibitorinhibitorinhibit

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IRAK4-IN-21

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IRAK4-IN-21 Related Antibodies

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Biological Activity

Purity & Documentation

References

Customer Review

IRAK4-IN-21 Related Antibodies

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Complete Stock Solution Preparation Table

IRAK4-IN-21 Related Classifications

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