2. Cell Cycle/DNA Damage
  3. PERK
  4. PERK-IN-5

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

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PERK-IN-5 Chemical Structure

PERK-IN-5 Chemical Structure

CAS No. : 2616821-91-9

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Based on 1 publication(s) in Google Scholar

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PERK-IN-5 Related Antibodies

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Description

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model[1].

IC50 & Target

IC50: 2 nM (PERK), 9 nM (p-eIF2α)[1]
In Vitro

PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PERK-IN-5 Related Antibodies
In Vivo

PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%[1].
PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD1 mice[1] (Pharmacokinetics)
Dosage: 3, 10, 30 and 100 mg/kg
Administration: p.o.; 0.25-24 hours
Result: Showed robust pharmacokinetics with Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%.
Animal Model: BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells)[1]
Dosage: 3 or 10 mg/kg
Administration: p.o.; twice daily, for 28 days
Result: Showed statistically significant tumor growth inhibition.
Molecular Weight

468.50

Formula

C25H26F2N4O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCC1=C(C2=CN=C(N)C(C(NC(C)C)=O)=C2)C=CC(NC([C@@H](C3=CC(F)=CC(F)=C3)O)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (533.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1345 mL 10.6724 mL 21.3447 mL
5 mM 0.4269 mL 2.1345 mL 4.2689 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1345 mL 10.6724 mL 21.3447 mL 53.3618 mL
5 mM 0.4269 mL 2.1345 mL 4.2689 mL 10.6724 mL
10 mM 0.2134 mL 1.0672 mL 2.1345 mL 5.3362 mL
15 mM 0.1423 mL 0.7115 mL 1.4230 mL 3.5575 mL
20 mM 0.1067 mL 0.5336 mL 1.0672 mL 2.6681 mL
25 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1345 mL
30 mM 0.0711 mL 0.3557 mL 0.7115 mL 1.7787 mL
40 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3340 mL
50 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0672 mL
60 mM 0.0356 mL 0.1779 mL 0.3557 mL 0.8894 mL
80 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6670 mL
100 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5336 mL
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PERK-IN-5 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PERK-IN-52616821-91-9PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseKinaseOrally bioavailable786-O cellEfficacyCancerSelectivityInhibitorinhibitorinhibit

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