KIRA6
- Product Name
- KIRA6
- CAS No.
- 1589527-65-0
- Chemical Name
- KIRA6
- Synonyms
- KIRA6;133808;CS-2625;IRE1 Inhibitor IV;KIRA6, 10 mM in DMSO;IRE1α Kinase Inhibiting RNase Attenuator 6;KIRA6;IRE1 INHIBITOR IV;IRE1Α KINASE INHIBITING RNASE ATTENUATOR 6;IRE1,Inhibitor,KIRA 6,KIRA6,KIRA-6,Inositol requiring enzyme 1,inhibit;1-(4-(8-Amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl);1-(4-(8-amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea
- CBNumber
- CB03054235
- Molecular Formula
- C28H25F3N6O
- Formula Weight
- 518.53
- MOL File
- 1589527-65-0.mol
KIRA6 Property
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:6.25(Max Conc. mg/mL);12.05(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);3.86(Max Conc. mM) - form
- A crystalline solid
- pka
- 13.13±0.43(Predicted)
- color
- off-white to brown
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- 19151
- Product name
- KIRA6
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 19151
- Product name
- KIRA6
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $142
- Updated
- 2024/03/01
- Product number
- 19151
- Product name
- KIRA6
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $213
- Updated
- 2024/03/01
- Product number
- 6687DW
- Product name
- 1-[4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea
- Packaging
- 10mg
- Price
- $334
- Updated
- 2021/12/16
- Product number
- CS-6901
- Product name
- KIRA6
- Purity
- 99.86%
- Packaging
- 1mg
- Price
- $50
- Updated
- 2021/12/16
KIRA6 Chemical Properties,Usage,Production
Uses
KIRA6 is an ATP-competitive IRE1α kinase inhibiting RNase attenuator (KIRA) that allosterically inhibits IRE1α RNase kinase activity (IC50 = 0.6 μM) and prevents oligomerization. It has been shown to inhibit IRE1α in vivo and to promote cell survival under ER stress. At 20 μg/ml, KIRA6 is reported to preserve photoreceptor functional viability in rat models of ER stress-induced retinal degeneration. At 5 mg/kg, it has also been shown to preserve pancreatic β cells, increase insulin, and reduce hyperglycemia in Akita diabetic mice.[Cayman Chemical]
Biological Activity
KIRA6 can inhibited KIT at a similar concentration range. Direct binding measurements revealed that GSK414 associated more tightly than KIRA6 to the KIT cytoplasmic domain. On the other hand, it probably through competitive binding protected KIT from GSK414-mediated degradation.
in vitro
In INS-1 cells, KIRA6 inhibits IRE1α auto-phosphorylation by Tg and XBP1 mRNA splicing by Tm in a dose-dependent manner.
in vivo
Intravitreally, KIRA6 preserves photoreceptor functional viability in rat models of ER stress-induced retinal degeneration. Systemically, KIRA6 preserves pancreatic β-cells, increases insulin, and reduces hyperglycemia in Akita diabetic mice. It inhibits IRE1α in vivo to preserve cell viability and function in diverse cells and rodent tissues experiencing ER stress. The pharmacokinetic profile of KIRA6 in BALB/c mice intraperitoneally (i.p.) dosed at 10 mg/kg shows good drug plasma AUC levels (AUC 0-24h = 14.3 μM*h) with moderate clearance (22.4 mL/min/kg). Drug half-life is 3.90 hours, Cmax is 3.3 μM, and plasma levels at 4 and 8hr are 1.2 μM and 0.33 μM, respectively.
KIRA6 Preparation Products And Raw materials
Raw materials
Preparation Products
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