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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
62 Results for "
PERK activator
" in MedChemExpress (MCE) Product Catalog:
Products (62)
62 Results for "PERK activator" in MCE Product Catalog:
163
163 Publications Verification
Synonyms: PD0325901; PD325901
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
43
43 Cited Publications
Research Areas:
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
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30 Cited Publications
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
9
9 Cited Publications
Target:
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MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .
8
8 Cited Publications
Target:
SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2
Research Areas:
SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .
3
BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer .
2
2 Cited Publications
Cat. No.: HY-B0168A
CAS No.: 101152-94-7
Target:
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Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
2
2 Cited Publications
Cat. No.: HY-B0168
CAS No.: 92623-85-3
Target:
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Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
1
1 Cited Publications
Cat. No.: HY-W050044
CAS No.: 2133-34-8
1
1 Cited Publications
HC-5404-Fu is an orally active PERK inhibitor with an IC50 of 0.001 μM against human PERK. HC-5404-Fu blocks PERK activation induced by VEGFR-TKI and disrupts the adaptive stress response triggered by VEGFR-TKI. HC-5404-Fu enhances anti-angiogenic effects by inhibiting newly formed and mature tumor blood vessels in renal cell carcinoma models. HC-5404-Fu can be used in research related to renal cell carcinoma .
Cat. No.: HY-159852
CAS No.: 2971769-60-3
BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
Cat. No.: HY-W010451
CAS No.: 533-73-3
Synonyms: Hydroxyhydroquinone
Cat. No.: HY-163985
CAS No.: 3099123-99-3
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model .
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
Synonyms: (S)-BAY 2965501
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer .
Research Areas:
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 .
Cat. No.: HY-P3136
CAS No.: 25849-90-5
Synonyms: TRV120055
Target:
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Cat. No.: HY-P3136A
Synonyms: TRV120055 hydrochloride
Target:
Research Areas:
Cat. No.: HY-W014937
CAS No.: 1137-42-4
Synonyms: 4HBP
Target:
Drug Metabolite PERK Eukaryotic Initiation Factor (eIF) NF-κB TNF Receptor Interleukin Related Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
4‑Hydroxybenzophenone (4HBP) is a major metabolite of Benzophenone (HY-Y0546) and is orally active. 4-Hydroxybenzophenone triggers endoplasmic reticulum stress and activates the PERK-eIF2α-ATF4-CHOP and IRE1α-XBP1s pathways, and inhibits IκB translation. 4-Hydroxybenzophenone induces endoplasmic reticulum stress, unfolded protein response activation, protein homeostasis imbalance, protein aggregation, oxidative stress, ROS accumulation, mitochondrial membrane potential decrease, ATP depletion, and cytotoxicity. 4-Hydroxybenzophenone induces neural stem cell apoptosis (apoptosis) and affects neuronal differentiation. 4-Hydroxybenzophenone promotes malignant proliferation of hepatocellular carcinoma cells and xenograft tumor growth in nude mice. 4-Hydroxybenzophenone can be used in research related to neurodevelopmental toxicity and hepatocellular carcinoma .
Cat. No.: HY-112903A
CAS No.: 2309756-20-3
YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer .
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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
