perk

AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) that induces autophagy. It also inhibits GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), making it useful for cancer research.

PERK-IN-2 is a potent inhibitor of PERK with an IC50 of 0.2 nM.

PERK-IN-3 is a potent inhibitor of PERK (IC50 of 7.4 nM).

GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells). GCN2-IN-6  is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9

CCT020312 (0-9 µM, 24 h) treatment of medium HT29 cells for 24 h resulted in a concentration-dependent loss of P-S608-pRB signaling with linear response values between 1.8 and 6.1 µM.

ISRIB is a potent and selective PERK inhibitor.

ONO-8130 is an orally available antagonist of EP1 receptor.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.

MK-28 is a selective PERK agonist that reduces toxicity and prolongs survival in a Huntington's disease model.MK-28 has a significant killing effect on MK28 gastric cancer cells.

PERK-IN-4 is a potent and selective PERK inhibitor with an IC50 value of 0.3 nM, used in the study of cancer and neurological disorders.

PERK-IN-6 is a novel and highly potent PERK inhibitor (IC50:2.5 nM).

(S)-PERK-IN-5, the S-enantiomer of PERK-IN-5, is a PERK inhibitor with an IC50 range of 0.101-0.250 μM.

PERK-IN-5 is a highly selective, potent, orally active inhibitor of protein kinase R-like endoplasmic reticulum (ER) kinase (PERK), displaying inhibition with IC50 values of 2 nM for PERK and 9 nM for p-eIF2α. PERK-IN-5 significantly inhibited tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.

GSK621 is a specific and potent AMPK activator.

BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor that induces pERK activation, and it can be utilized in cancer research.

IACS-13909 (BBP-398), a specific and potent allosteric inhibitor of SHP2, that suppresses signaling through the MAPK pathway.

Compound V8 (PERK/eIF2α activator 1), a flavonoid, exhibits anti-tumor properties by inducing apoptosis and activating the PERK-eIF2α-ATF4 pathway. It effectively inhibits the proliferation of HepG2 cells, with an IC 50 value of 23 μM [1].

Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis.

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.