1. Cell Cycle/DNA Damage
  2. IRE1
  3. Kira8

Kira8 (Synonyms: AMG-18)

Cat. No.: HY-114368 Purity: 99.74%
Handling Instructions

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

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

Kira8 Chemical Structure

Kira8 Chemical Structure

CAS No. : 1630086-20-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 291 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
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10 mg USD 350 In-stock
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50 mg USD 1100 In-stock
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100 mg USD 1600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM[1].

IC50 & Target

IRE1α[1]
IC50: 5.9 nM (IRE1α RNase)[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].

In Vivo

Male Ins2+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks[1].
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs[1].

Animal Model: Male Ins2+/Akita mice[1]
Dosage: 50 mg/kg
Administration: Injected i.p.; daily; for 35 days
Result: Significant reduction of hyperglycemia became apparent over several weeks.
Molecular Weight

601.12

Formula

C₃₁H₂₉ClN₆O₃S

CAS No.

1630086-20-2

SMILES

O=S(C1=CC=CC=C1Cl)(NC2=C3C=CC(C)=C(OC4=NC=CC=C4C5=NC(N[[email protected]@H]6CNCCC6)=NC=C5)C3=CC=C2)=O

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 : 65 mg/mL (108.13 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6636 mL 8.3178 mL 16.6356 mL
5 mM 0.3327 mL 1.6636 mL 3.3271 mL
10 mM 0.1664 mL 0.8318 mL 1.6636 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (3.61 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Kira8
Cat. No.:
HY-114368
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