2. Immunology/Inflammation Cell Cycle/DNA Damage
  3. IRAK CDK
  4. HS-243

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.

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

HS-243 Chemical Structure

HS-243 Chemical Structure

CAS No. : 848249-10-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 240 In-stock
25 mg USD 480 In-stock
50 mg USD 820 In-stock
100 mg USD 1300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

HS-243 Related Antibodies

Top Publications Citing Use of Products

View All IRAK Isoform Specific Products:

View All Isoforms
IRAK1 IRAK4

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

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Description

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity[1].

IC50 & Target

IRAK4

20 nM (IC50)

IRAK-1

24 nM (IC50)

CLK4

662 nM (IC50)

In Vitro

HS-243 (0-10 μM, 24 h) inhibits cell survival by 21% for AN3-CA (pancreatic cancer cell), and 13% for SKOV-3 (ovarian cancer cell)[1].
HS-243 (10 μM, 24 h) potently reduces the proinflammatory response of RA cells and macrophages, significantly reduces the secretion of 15 cytokines, including IL-8, CD14, GRO-α, MIP-1a, MIP-3a, uPAR, Osteopontin, MMP-9, MCP-1, I-TAC, TIM-3, IP-10, GDF-15, and RANTES[1].
HS-243 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM[1].

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

HS-243 Related Antibodies

Cell Viability Assay[1]

Cell Line: SK-OV-3, AN3-CA, H460, ES-2, SK-UT-1B, COLO205, Bx-PC-3
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, and 10 μM+IL-1β (30 ng/ml)
Incubation Time: 24 h
Result: Inhibited cell survival by 21% for AN3-CA (pancreatic), and 13% for SKOV-3 (ovarian). The addition of IL-1β in conjunction with HS-243 increased cell death to 46% in SK-OV-3 (ovarian), 33% in AN3-CA (pancreatic), and 31% in H460 (colon).
Molecular Weight

324.33

Formula

C17H16N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC2=CC=CC=C2N1CCC)C3=CC=CC([N+]([O-])=O)=C3
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 : 41.67 mg/mL (128.48 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 3.0833 mL 15.4164 mL 30.8328 mL
5 mM 0.6167 mL 3.0833 mL 6.1666 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.

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Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0833 mL 15.4164 mL 30.8328 mL 77.0820 mL
5 mM 0.6167 mL 3.0833 mL 6.1666 mL 15.4164 mL
10 mM 0.3083 mL 1.5416 mL 3.0833 mL 7.7082 mL
15 mM 0.2056 mL 1.0278 mL 2.0555 mL 5.1388 mL
20 mM 0.1542 mL 0.7708 mL 1.5416 mL 3.8541 mL
25 mM 0.1233 mL 0.6167 mL 1.2333 mL 3.0833 mL
30 mM 0.1028 mL 0.5139 mL 1.0278 mL 2.5694 mL
40 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9270 mL
50 mM 0.0617 mL 0.3083 mL 0.6167 mL 1.5416 mL
60 mM 0.0514 mL 0.2569 mL 0.5139 mL 1.2847 mL
80 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9635 mL
100 mM 0.0308 mL 0.1542 mL 0.3083 mL 0.7708 mL
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HS-243 Related Classifications

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:

HS-243848249-10-5HS243HS 243IRAKCDKInterleukin-1 receptor associated kinaseIL-1R associated kinaseCyclin dependent kinaseTHP-1RA-FLSsSK-OV-3AN3-CAH460immunologyrheumatoid arthritisautoimmune diseaseinterleukintumor necrosis factorTNFanti-inflammatoryInterleukin-1 receptor associated kinase-1Inhibitorinhibitorinhibit

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