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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
52 Results for "
Pkr
" in MedChemExpress (MCE) Product Catalog:
Products (52)
52 Results for "Pkr" in MCE Product Catalog:
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TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR .
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8 Cited Publications
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PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions .
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Dimethyl biphenyl-4,4'-dicarboxylate (Biphenyl dimethyl dicarboxylate) is a hepatoprotective agent. Dimethyl biphenyl-4,4'-dicarboxylate stimulates the Jak/Stat signaling pathway and induces the expression of IFN-α-stimulated genes, particularly 6-16 and ISG12. Dimethyl biphenyl-4,4'-dicarboxylate inhibits the replication of pregenomic RNA and HBeAg. Polymer micelles loaded with Dimethyl biphenyl-4,4'-dicarboxylate can serve as carriers for the compound. Dimethyl biphenyl-4,4'-dicarboxylate can be used as an auxiliary improving agent for chronic hepatitis. Dimethyl biphenyl-4,4'-dicarboxylate is applicable to research related to chronic hepatitis B .\n
Synonyms: PkrA7
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PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. .
Cat. No.: HY-101997
CAS No.: 455311-98-5
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BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) modulator. BEPP hydrochloride enhances the phosphorylation levels of PKR and eIF2α, activates caspase-3, upregulates the pro-apoptotic protein BAX, and downregulates the anti-apoptotic protein Bcl-2. BEPP hydrochloride inhibits vaccinia virus replication and exhibits selective cytotoxicity in cells expressing PKR. BEPP hydrochloride can be used in research related to cancer and viral infections .
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PKR-IN-C51 is an ATP-competitive protein kinase R (PKR) inhibitor with a human IC50 of 9 μM and a human Ki of 3.4 μM. PKR-IN-C51 blocks the activation of PKR, inhibits intracellular PKR activation in primary mouse macrophages, and shows no obvious cytotoxicity. PKR-IN-C51 can be used in studies related to the regulation of PKR-mediated signaling pathways .
Synonyms: AG-946; Pkr activator 2
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Tebapivat (PKR activator 2) is a potent pyruvate kinase-R (PKR) activator extracted from patent WO2019035863A1, compound 385 .
Cat. No.: HY-W010451
CAS No.: 533-73-3
Synonyms: Hydroxyhydroquinone
Synonyms: FT-4202
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Etavopivat is a potent, selective, and orally active erythrocyte pyruvate kinase (PKR) activator. Etavopivat has potent antisickling effects that can be used in studies of sickle cell disease and other haemoglobinopathies .
Cat. No.: HY-W319647
CAS No.: 315705-10-3
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GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC50 of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD) .
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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 .
Cat. No.: HY-19702
CAS No.: 1628428-01-2
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PKR activator 3 (Compound 160) is a red blood cell pyruvate kinase (PKR) activator. PKR activator 3 can be used in the research of diseases related to PKR function, such as pyruvate kinase deficiency (PKD) .
Synonyms: 7-Desacetoxy-6,7-dehydrogedunin
Target:
PERK Prokineticin Receptor P2X Receptor Caspase NOD-like Receptor (NLR) Pyroptosis Tyrosinase
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders .
Cat. No.: HY-159972
CAS No.: 910113-60-9
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PKR1 antagonist 1 (PC1) is a potent PKR1 antagonist. PKR1 antagonist 1 reduces hyperalgesia and allodynia in SNI mice .
Cat. No.: HY-175880
CAS No.: 1644664-11-8
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AMG-34 is a GCN2-targeting agent with IC50 values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, PERK, HRland PKR, respectively .
Cat. No.: HY-153354
CAS No.: 2283420-05-1
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PKR activator 4 (example 7A) is a potent pyruvate kinase R (PKR) activator. PKR activator 4 has the potential for the research of blood disorders .
Synonyms: (Rac)-FT-4202
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(Rac)-Etavopivat ((Rac)-FT-4202) is an isomer of Etavopivat (HY-139573). Etavopivat is an orally active erythrocyte pyruvate kinase-R (PKR) activator that can be used in studies of sickle cell disease and other haemoglobinopathies .
Cat. No.: HY-168446
CAS No.: 3057531-75-3
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PKR-IN-1 (Compound 5s) is a pyruvate kinase (PK) inhibitor that has antifungal activity, with an EC50 of 0.21 μg/mL for R. solani .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
