2. Cell Cycle/DNA Damage
  3. IRE1
  4. Kira8 Hydrochloride

Kira8 Hydrochloride  (Synonyms: AMG-18 Hydrochloride)

Cat. No.: HY-114368A Purity: 98.03%
COA
SDS
Handling Instructions Technical Support

Kira8 Hydrochloride (AMG-18 Hydrochloride) 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.

CAS No. : 2250019-92-0

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg Get quote
100 mg Get quote
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Kira8 Hydrochloride:

Kira8 Hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670.  [Abstract]

    FXBP1s expression. Western immunoblot of hSAECs transduced with empty (pCT) or FXBP1s-expressing lentiviral vector at an MOI of 2.0 for 48 h, or mock-treated or treated with tunicamycin (TM, 0.5 μg/ml for 8 h) or thapsigargin (Tg, 50 nM for 6 h) in the absence or presence of KIRA8 (10 μM). Nuclear extracts were prepared and stained with anti-FLAG M2 or anti-XBP1s antibodies. TBP was used as loading control.

    Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2023 May 8;51(8):3650-3670.  [Abstract]

    We observed that Tg induced a 3.5 ± 0.5-fold increase in endogenous XBP1s binding to the GFPT1 promoter. This induction was completely inhibited by the treatment with KIRA8 (10 μM).

    Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000.

    In a manner similar to our observations on the RSV induction of cell-associated FN1, we found that FN1 deposition into the ECM was also blocked by KIRA8 (10 μM, pre-treated for two hours).

    Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000.

    Principal component analysis of significant proteins (ANOVA with permutation-based FDR < 0.01). Green circle, controls; red square, RSV infection; blue diamond, RSV infection + KIRA8 treatment.

    Kira8 Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 12;23(16):9000.

    Proteomics analysis of N-glycosylation in hSAECs infected with RSV in the presence or absence of KIRA8. hSAECs were infected with RSV at 1.0 MOI for 24 h in the presence or absence of KIRA8 (10 µM). The N-glycosylated peptides were enriched with lectins and then analyzed with label-free LC-MS/MS. Volcano plot of N-glycosylated peptides (RSV vs. Control). Red circle, N-glycoproteins upregulated by RSV; green square, N-glycoproteins downregulated by RSV infection.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Kira8 Hydrochloride (AMG-18 Hydrochloride) 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].

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

    Kira8 Hydrochloride Related Antibodies
    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].

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

    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

    637.58

    Formula

    C31H30Cl2N6O3S
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    H2O : ≥ 100 mg/mL (156.84 mM)

    DMSO : 50 mg/mL (78.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5684 mL 7.8422 mL 15.6843 mL
    5 mM 0.3137 mL 1.5684 mL 3.1369 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.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    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 / H2O 1 mM 1.5684 mL 7.8422 mL 15.6843 mL 39.2108 mL
    5 mM 0.3137 mL 1.5684 mL 3.1369 mL 7.8422 mL
    10 mM 0.1568 mL 0.7842 mL 1.5684 mL 3.9211 mL
    15 mM 0.1046 mL 0.5228 mL 1.0456 mL 2.6141 mL
    20 mM 0.0784 mL 0.3921 mL 0.7842 mL 1.9605 mL
    25 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5684 mL
    30 mM 0.0523 mL 0.2614 mL 0.5228 mL 1.3070 mL
    40 mM 0.0392 mL 0.1961 mL 0.3921 mL 0.9803 mL
    50 mM 0.0314 mL 0.1568 mL 0.3137 mL 0.7842 mL
    60 mM 0.0261 mL 0.1307 mL 0.2614 mL 0.6535 mL
    H2O 80 mM 0.0196 mL 0.0980 mL 0.1961 mL 0.4901 mL
    100 mM 0.0157 mL 0.0784 mL 0.1568 mL 0.3921 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Kira8 Hydrochloride 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:

    Kira82250019-92-0AMG-18Kira 8Kira-8AMG18AMG 18IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Kira8 Hydrochloride
    Cat. No.:
    HY-114368A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (254 KB) Français - FR (254 KB) Deutsch - DE (254 KB) Norwegian - NO (254 KB) Español - ES (254 KB) Swedish - SV (254 KB) Italian - IT (254 KB) Korean - KR (254 KB) Portuguese - PT (254 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.