BiochemicalTargets

UPR

The unfolded protein response (UPR), a wide-ranging process overseen by the endoplasmic reticulum (ER), regulates basal and acute cellular function. It entails maintenance of protein homeostasis through removal of unfolded (or misfolded) proteins and affects processes as diverse as lipid and glucose metabolism and innate immunity. Under normal conditions, buildup of unfolded proteins is detected by activating transcription factor 6 (ATF6), inositol-requiring protein 1 (IRE1), and protein kinase RNA-like ER kinase (PERK), triggering the ER stress response, including UPR. Chronic activation of these pathways can lead to cancer, neurodegeneration, and metabolic diseases.

PERK

GSK2606414 | PERK inhibitor

GSK2606414 (1337531-36-8) is a potent (IC50 = 0.4 nM) and selective (against a panel of 294 kinases) inhibitor of protein kinase R-like endoplasmic reticulum kinase (PERK), an

eIF2

YM-58483 | CRAC channel blocker

CAS:
223499-30-7
Catalog Number:
10-2935
Activity:
CRAC channel blocker
Chemical Names:
N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Alternate Name:
BTP2
Molecular Weight:
421.32
Molecular Formula:
C15H9F6N5OS
Solubility:
Soluble in DMSO (40 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Manidipine dihydrochloride | Calcium channel blocker

CAS:
89226-75-5
Catalog Number:
10-2045
Activity:
Calcium channel blocker
Chemical Names:
5-O-[2-(4-Benzhydrylpiperazin-1-yl)ethyl] 3-O-methyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate dihydrochloride
Alternate Name:
CV-4093
Molecular Weight:
683.63
Molecular Formula:
C35H38N4O6·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
Room temperature
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Nimodipine | L-type calcium channel blocker

CAS:
66085-59-4
Catalog Number:
10-1321
Activity:
L-type calcium channel blocker
Chemical Name:
1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methyloxyethyl 1-methylethyl ester
Alternate Names:
BAY-e 9736
Molecular Weight:
418.44
Molecular Formula:
C21H26N2O7
Solubility:
Soluble in DMSO (up to 40 mg/ml)
Physical Properties:
Pale-yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

ATF6

Repaglinide | Kir6 blocker

Repaglinide (135062-02-1) is a blocker of the ATP-sensitive potassium channel Kir6 with hypoglycemic activity.1 Clinically useful antidiabetic agent. It displays 30-fold selectivity for pancreatic Kir6.2/SUR1 over