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PKRA83 hydrochloride  (Synonyms: PKRA7 hydrochloride)

Cat. No.: HY-147056B
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PKRA83 (PKRA7) hydrochloride is a potent, blood-brain-penetrating PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities.

For research use only. We do not sell to patients.

PKRA83 hydrochloride

PKRA83 hydrochloride Chemical Structure

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PKRA83 hydrochloride Related Antibodies

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Description

PKRA83 (PKRA7) hydrochloride is a potent, blood-brain-penetrating PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities[1].

IC50 & Target

IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]
In Vitro

PKRA83 (1 µg/mL) hydrochloride effectively reduces PK2-induced microvascular endothelial cell branching in vitro[1].
PKRA83 (2 μM, 24 h) hydrochloride blocks the neuroprotective action of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cell against MPP+-induced dopaminergic neuronal cell death)[3].

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

PKRA83 hydrochloride Related Antibodies
In Vivo

PKRA83 (20 mg/kg; i.p) hydrochloride shows anti-tumor activity in the context of glioblastoma xenograft tumor models[1].
PKRA83 (15 mg/kg; i.p, daily for 2 weeks) hydrochloride inhibits arthritis in mice with collagen-induced arthritis[2].

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

Animal Model: glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
Dosage: 20 mg/kg
Administration: i.p, daily
Result: Decreased tumor growth rate and tumor weight.
Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
Animal Model: Collagen-induced arthritis in mice[2]
Dosage: 15 mg/kg
Administration: i.p, daily for 2 weeks
Result: Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).
Lowered IL-1β and 1 L-6 gene expression levels in the joints.
Molecular Weight

541.48

Formula

C27H35Cl2FN2O4
SMILES

ClC1=C2C(OCCCO2)=CC(CN(CC(C)C)C([C@H]3CN(CC3)CC4=CC(OC)=C(C=C4)F)=O)=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PKRA83 hydrochloride Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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:

PKRA83PKRA7PKRA 83PKRA-83PKRA 7PKRA-7OthersprokineticinPKR1PKR2anticanceranti-angiogenic activitiesblood-brain barrierarthritisInhibitorinhibitorinhibit

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