1. Immunology/Inflammation Cell Cycle/DNA Damage
  2. IRAK CDK
  3. 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.

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HS-243

HS-243 構造式

CAS 番号 : 848249-10-5

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 154 在庫あり
Solution
10 mM * 1 mL in DMSO USD 154 在庫あり
Solid
5 mg $140 在庫あり
10 mg $240 在庫あり
25 mg $480 在庫あり
50 mg $705 在庫あり
100 mg $1010 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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)

体外実験

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.

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).
分子量

324.33

分子式

C17H16N4O3

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC2=CC=CC=C2N1CCC)C3=CC=CC([N+]([O-])=O)=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.3083 mL 1.5416 mL 3.0833 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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純度とドキュメンテーション
参考文献

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

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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.

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Inquiry Information

製品名:
HS-243
製品番号:
HY-134911
数量:
MCE 日本正規代理店: