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Kira8

  Cat. No.:  DC20111   Featured
Chemical Structure
1630086-20-2
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More than 5000 active chemicals with high quality for research!
Field of application
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1630086-20-2
SMILES: CC1=C(C2=C(C=C1)C(=CC=C2)NS(=O)(=O)C3=CC=CC=C3Cl)OC4=C(C=CC=N4)C5=NC(=NC=C5)N[C@H]6CCCNC6
Formula: C31H29ClN6O3S
M.Wt: 601.12
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8.
Description: In Vitro KIRA8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. KIRA8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2. In Vivo Kira8 efficaciously reverses established diabetes in NOD mice by sparing β-cells and preserving their physiological function. KIRA8 is first tested in 3-week-old male pre-diabetic Akita mice by i.p. daily dosing of 50 mg/kg, whereupon significant reduction of hyperglycemia became apparent over several weeks. Then KIRA8 (50 mg/kg) is tested in the complex NOD. Showing target engagement, one week treatment of pre-diabetic NODs with KIRA8 leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserved Ins1/Ins2, BiP and MANF mRNAs.
Target: IRE1α[1]
In Vivo: Kira8 efficaciously reverses established diabetes in NOD mice by sparing β-cells and preserving their physiological function. KIRA8 is first tested in 3-week-old male pre-diabetic Akita mice by i.p. daily dosing of 50 mg/kg, whereupon significant reduction of hyperglycemia became apparent over several weeks. Then KIRA8 (50 mg/kg) is tested in the complex NOD. Showing target engagement, one week treatment of pre-diabetic NODs with KIRA8 leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserved Ins1/Ins2, BiP and MANF mRNAs[1].
In Vitro: KIRA8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. KIRA8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2[1].
References: [1]. Morita S, et al. Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes. Cell Metab. 2017 Apr 4;25(4):883-897.e8.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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