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KIRA6

CAS No.
1589527-65-0
Chemical Name:
KIRA6
Synonyms
KIRA6;133808;CS-2625;IRE1 Inhibitor IV;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;Urea, N-[4-[8-amino-3-(1,1-dimethylethyl)imidazo[1,5-a]pyrazin-1-yl]-1-naphthalenyl]-N'-[3-(trifluoromethyl)phenyl]-
CBNumber:
CB03054235
Molecular Formula:
C28H25F3N6O
Molecular Weight:
518.53
MDL Number:
MFCD29477497
MOL File:
1589527-65-0.mol
Last updated:2023-05-21 10:59:17

KIRA6 Properties

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)

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H335-H319-H315
Precautionary statements  P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362

KIRA6 price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 19151 KIRA6 ≥98% 1589527-65-0 1mg $37 2024-03-01 Buy
Cayman Chemical 19151 KIRA6 ≥98% 1589527-65-0 5mg $142 2024-03-01 Buy
Cayman Chemical 19151 KIRA6 ≥98% 1589527-65-0 10mg $213 2024-03-01 Buy
AK Scientific 6687DW 1-[4-(8-Amino-3-tert-butylimidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl]-3-[3-(trifluoromethyl)phenyl]urea 1589527-65-0 10mg $334 2021-12-16 Buy
ChemScene CS-6901 KIRA6 99.86% 1589527-65-0 1mg $50 2021-12-16 Buy
Product number Packaging Price Buy
19151 1mg $37 Buy
19151 5mg $142 Buy
19151 10mg $213 Buy
6687DW 10mg $334 Buy
CS-6901 1mg $50 Buy

KIRA6 Chemical Properties,Uses,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

KIRA6 Suppliers

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1-(4-(8-amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl)phenyl)urea 1-(4-(8-Amino-3-(tert-butyl)imidazo[1,5-a]pyrazin-1-yl)naphthalen-1-yl)-3-(3-(trifluoromethyl) CS-2625 IRE1 Inhibitor IV IRE1α Kinase Inhibiting RNase Attenuator 6 KIRA6;IRE1 INHIBITOR IV;IRE1Α KINASE INHIBITING RNASE ATTENUATOR 6 133808 3-(4-{8-amino-3-tert-butyl-1H,7H-imidazo[1,5-a]pyrazin-1-ylidene}-1,4-dihydronaphthalen-1-ylidene)-1-[3-(trifluoromethyl)phenyl]urea Urea, N-[4-[8-amino-3-(1,1-dimethylethyl)imidazo[1,5-a]pyrazin-1-yl]-1-naphthalenyl]-N'-[3-(trifluoromethyl)phenyl]- KIRA6 IRE1,Inhibitor,KIRA 6,KIRA6,KIRA-6,Inositol requiring enzyme 1,inhibit 1589527-65-0 API