Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. PERK is implicated in tumorigenesis and cancer cell survival. GSK2606414 is an orally available, potent, and selective PERK inhibitor. GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. PERK activation is independent of the large increase in unfolded nascent proteins within the ER following transient global brain ischemia.


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GSK143

GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].

  • CAS Number: 1240390-27-5
  • MF: C17H22N6O2
  • MW: 342.39600
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S)-JDQ-443

(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity[1][2].

  • CAS Number: 2653994-10-4
  • MF: C29H28ClN7O
  • MW: 526.03
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG PERK 44

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively[1][2].

  • CAS Number: 1883548-84-2
  • MF: C34H29ClN4O2
  • MW: 561.07
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MEK/PI3K-IN-1

MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines[1].

  • CAS Number: 2281803-28-7
  • MF: C36H37F5IN9O6
  • MW: 913.63
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PERK-IN-2

PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM[1].

  • CAS Number: 1337531-83-5
  • MF: C23H18F3N5O
  • MW: 437.42
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-28

MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1].

  • CAS Number: 864388-65-8
  • MF: C24H20N4O2
  • MW: 396.44
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-{4-[(4-Chloro-1-piperidinyl)sulfonyl]phenyl}-5-nitro-2-furamide

ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden[1].

  • CAS Number: 1523437-16-2
  • MF: C16H16ClN3O6S
  • MW: 413.83
  • Catalog: Apoptosis
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7DG

7DG (7-Desacetoxy-6,7-dehydrogedunin) is a selective inhibitor of protein kinase R (PKR) that directly interact with the C-terminal of PKR; completely protectes macrophages from anthrax lethal toxin (LT)-induced pyroptotic cell death, a model for inflammasome-mediated caspase-1 activation, with an (IC50) of 5 uM.

  • CAS Number: 26927-01-5
  • MF: C26H30O5
  • MW: 422.51
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NBI42902

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1].

  • CAS Number: 352290-60-9
  • MF: C27H24F3N3O3
  • MW: 495.49
  • Catalog: PERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 631.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 335.4±34.3 °C

PERK-IN-4

PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].

  • CAS Number: 1337531-89-1
  • MF: C24H19F4N5O
  • MW: 469.434
  • Catalog: PERK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 710.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 383.7±32.9 °C

LUF 6283

LUF6283 is a potent and orally active HCA(2) partial agonist, with a Ki of 0.55 µM. LUF6283 can achieve the beneficial lipid lowering effect of niacin without producing the unwanted cutaneous flushing side effect[1].

  • CAS Number: 92933-48-7
  • MF: C8H12N2O2
  • MW: 168.19300
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PERK-IN-6

PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM[1].

  • CAS Number: 1337532-14-5
  • MF: C23H22N6O
  • MW: 398.46
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VU 0424465

VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons[1][2].

  • CAS Number: 1428630-85-6
  • MF: C19H19FN2O2
  • MW: 326.36
  • Catalog: PERK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 533.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 276.7±30.1 °C

MEK/PI3K-IN-2

MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines[1].

  • CAS Number: 2281803-33-4
  • MF: C38H41F5IN9O7
  • MW: 957.68
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ONO 8130

ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research[1].

  • CAS Number: 459841-96-4
  • MF: C25H28N2O5S2
  • MW: 500.63
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Derrone

Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity[1][2].

  • CAS Number: 76166-59-1
  • MF: C20H16O5
  • MW: 336.34
  • Catalog: Aurora Kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 584.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 214.6±23.6 °C

HC-5404

HC-5404 is a potent and selective PERK inhibitor. HC-5404 has orally activity. HC-5404 significantly blocks metastasis via killing quiescent/slow-cycling ISRhigh[1][2].

  • CAS Number: 2247396-91-2
  • MF: C24H24F2N4O3
  • MW: 454.47
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ISRIB

ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.

  • CAS Number: 1597403-47-8
  • MF: C22H24Cl2N2O4
  • MW: 451.343
  • Catalog: PERK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 719.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 388.6±32.9 °C

GSK2656157

GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.

  • CAS Number: 1337532-29-2
  • MF: C23H21FN6O
  • MW: 416.451
  • Catalog: PERK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 744.6±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 404.1±32.9 °C

PERK-IN-3

PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM[1].

  • CAS Number: 1337532-08-7
  • MF: C22H16F2N4O2
  • MW: 406.38
  • Catalog: PERK
  • Density: 1.446±0.06 g/cm3(Predicted)
  • Boiling Point: 694.8±55.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

GSK2606414

GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM.

  • CAS Number: 1337531-36-8
  • MF: C24H20F3N5O
  • MW: 451.444
  • Catalog: PERK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 720.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 389.4±32.9 °C

GSK143 dihydrochloride

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].

  • CAS Number: 2341796-81-2
  • MF: C17H24Cl2N6O2
  • MW: 415.32
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MSU-42011

MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research[1].

  • CAS Number: 2456434-36-7
  • MF: C24H34N2O2
  • MW: 382.54
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC 295642

NSC 295642 is a phosphatase inhibitor. NSC 295642 can significantly increase phospho-Erk cytonuclear differences in intact cells. NSC 295642 can be used for the research of cancer[1].

  • CAS Number: 77111-29-6
  • MF: C15H14ClCuN3S2
  • MW: 399.42100
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S)-PERK-IN-5

(S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM[1][2].

  • CAS Number: 2616821-92-0
  • MF: C25H26F2N4O3
  • MW: 468.50
  • Catalog: PERK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCT020312

CCT020312 is capable of delivering potent, and eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, proliferation control and also is an activator of RNA-like endoplasmic reticulum kinase (PERK).

  • CAS Number: 324759-76-4
  • MF: C31H30Br2N4O2
  • MW: 650.40
  • Catalog: Eukaryotic Initiation Factor (eIF)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Takeda-6d

Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity[1].

  • CAS Number: 1125632-93-0
  • MF: C27H19ClFN5O3S
  • MW: 547.988
  • Catalog: PERK
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A