GSI526
GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.
(Pink: IRAK4 ligand (HY-183800); Blue: VHL ligand (HY-112078); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C51H62N10O7S
- 分子量:959.17
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
|
VHL |
IRAK4 |
GSI526 (1-10000 nM; 24 h) induces dose-dependent degradation of IRAK4 in HEK293T cells with a DC50 of 50.89 nM and a Dmax greater than 80%[1].
GSI526 (0.01-30 μM; 24 h) exhibits no cytotoxicity in THP-1 cells at concentrations up to 30 μM following 24 h incubation[1].
GSI526 (0.01-30 μM; 48 h) exhibits no cytotoxicity in HEK293T cells at concentrations up to 30 μM following 48 h incubation[1].
GSI526 (1000 nM; 8 h) exhibits marked selectivity toward IRAK4 in THP-1 cells, with IRAK4 showing a statistically significant downregulation following 8 h treatment with 1000 nM GSI526[1].
GSI526 (1-5 μM; 1 h pretreatment, followed by 6 h LPS stimulation) inhibits LPS-induced activation of the IRAK4-NF-κB/MAPK signaling pathway in THP-1 cells via degradation of IRAK4[1].
GSI526 (0.3-3 μM; 1 h pretreatment, followed by 24 h LPS stimulation) dose-dependently inhibits LPS-induced expression of TNF-α and CXCL8 in THP-1 cells via suppression of the IRAK4-NF-κB/MAPK signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:THP-1 human monocytic leukemia cells
-
Concentration:1-10000 nM (dose-response); 1 μM (time-course)
-
Incubation Time:24 h (dose-response); 2-24 h (time-course)
-
Result:Induced dose-dependent degradation of IRAK4 with a DC50 of 40.17 nM and a maximum degradation (Dmax) of 97%.
Resulted in detectable IRAK4 degradation within 2 h, with maximal degradation achieved by 8 h, and the degradative effect was sustained for up to 24 h.
-
Cell Line:HEK293T human embryonic kidney cells
-
Concentration:1-10000 nM
-
Incubation Time:24 h
-
Result:Induced dose-dependent degradation of IRAK4 with a DC50 of 50.89 nM and a Dmax greater than 80%.
-
Cell Line:THP-1 human monocytic leukemia cells
-
Concentration:0.01-30 μM
-
Incubation Time:24 h
-
Result:Did not induce cytotoxic cell death at concentrations up to 30 μM.
-
Cell Line:HEK293T human embryonic kidney cells
-
Concentration:0.01-30 μM
-
Incubation Time:48 h
-
Result:Did not induce cytotoxic cell death at concentrations up to 30 μM.
-
Cell Line:THP-1 human monocytic leukemia cells
-
Concentration:1-5 μM
-
Incubation Time:1 h pretreatment, followed by 6 h LPS stimulation
-
Result:Inhibited LPS-induced phosphorylation of JNK, p38, ERK, and p65 (NF-κB) in a concentration-dependent manner via IRAK4 degradation.
-
Cell Line:THP-1 human monocytic leukemia cells
-
Concentration:0.3-3 μM
-
Incubation Time:1 h pretreatment, followed by 24 h LPS stimulation
-
Result:Significantly inhibited LPS-induced secretion of pro-inflammatory cytokine TNF-α and chemokine CXCL8, with the inhibitory effect particularly evident at 1 and 3 μM.
化学情報
-
分子量 959.17
-
分子式 C51H62N10O7S
-
SMILES
O=C(C1=NC(C2=CC=NN2)=CC=C1)NC3=C(OC)C=C(N4CCC5(CN(C(CCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(N[C@@H](C)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)=O)C5)CC4)C=C3
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
GSI526 関連分類
HY-183799 関連分類
Powered by Bioz