MedKoo Cat#: 574716 | Name: PERK-IN-4
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PERK-IN-4 is an inhibitor of PERK, an important transmembrane protein of endoplasmic reticulum (ER). GSK PERK Inhibitor can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways. As a result, GSK PERK Inhibitor has potential use in the treatment of diseases such as Alzheimer's disease, stroke, Type 1 diabetes, Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung.

Chemical Structure

PERK-IN-4
CAS#1337531-89-1

Theoretical Analysis

MedKoo Cat#: 574716

Name: PERK-IN-4

CAS#: 1337531-89-1

Chemical Formula: C24H19F4N5O

Exact Mass: 469.1526

Molecular Weight: 469.44

Elemental Analysis: C, 61.41; H, 4.08; F, 16.19; N, 14.92; O, 3.41

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
3-Fluoro-GSK2606414; 3-Fluoro-GSK 2606414; 3-Fluoro-GSK-2606414; PERK-IN-4; PERK-inhibitor-4
IUPAC/Chemical Name
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone
InChi Key
PXVQGBJMIQCDEX-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H19F4N5O/c1-32-11-18(21-22(29)30-12-31-23(21)32)14-2-3-19-15(9-14)4-5-33(19)20(34)8-13-6-16(24(26,27)28)10-17(25)7-13/h2-3,6-7,9-12H,4-5,8H2,1H3,(H2,29,30,31)
SMILES Code
FC(C1=CC(F)=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3)=O)=C1)(F)F
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
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.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM comments
Solubility
DMSO 90.0 191.72
Ethanol 21.0 44.73
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 469.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1.Wu MS, Chien CC, Jargalsaikhan G, Ilsan NA, Chen YC. Activation of PERK Contributes to Apoptosis and G2/M Arrest by Microtubule Disruptors in Human Colorectal Carcinoma Cells ‡. Cancers (Basel). 2019;12(1):97. Published 2019 Dec 30. doi:10.3390/cancers12010097