Scientific Reviews
Product Guides
Blogs
Topics
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
20 Results for "
pERK inhibition
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "pERK inhibition" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: EGFR mutant-IN-3
Target:
Forschungsgebiete:
NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR WT with an IC50 of 0.4 nM. NT-1 also inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M. NT-1 exerts deeper inhibition on p-EGFR and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research .
Art. -Nr.: HY-159852
CAS. Nr.: 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 .
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
Art. -Nr.: HY-146544
CAS. Nr.: 2230873-78-4
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146223
Reinheit: 99.52%
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
Art. -Nr.: HY-146543
CAS. Nr.: 2230873-96-6
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146476
CAS. Nr.: 2230873-66-0
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146533
CAS. Nr.: 2230874-00-5
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146223A
Reinheit: 98.00%
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
Art. -Nr.: HY-146475
CAS. Nr.: 2230873-65-9
KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146545
CAS. Nr.: 2230873-75-1
KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146546
CAS. Nr.: 2230873-67-1
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-146537
CAS. Nr.: 2253119-24-1
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers .
Art. -Nr.: HY-170849
Forschungsgebiete:
Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
Art. -Nr.: HY-181704
CAS. Nr.: 3084918-70-4
KRAS-IN-54 is a macrocyclic KRAS inhibitor. KRAS-IN-54 exhibits activity against cell viability and pERK inhibition in cells with KRAS G12D and KRAS G13D mutations. KRAS-IN-54 can be used in the research of KRAS-mutant cancers, including pancreatic adenocarcinoma, colorectal cancer, non-small cell lung cancer, esophageal cancer, gallbladder cancer, melanoma, ovarian cancer and endometrial cancer .
Art. -Nr.: HY-134800
CAS. Nr.: 692744-81-3
IBT21 is an endoplasmic reticulum stress inhibitor that binds to unfolded or misfolded proteins and prevents their aggregation. IBT21 inhibits UPR activation of the ATF6, IRE1 and PERK branches under ER stress, with IC50 values of 0.24 μM, 0.33 μM, and 0.46 μM, respectively. IBT21 protects cells from ER stress-induced death and mutant prion protein (protein toxin)-induced growth inhibition. IBT21 exhibits chemical chaperone activity distinct from UPR modulators, does not affect protein translation, moderately reduces DTT (HY-15917)-induced ER stress, and fails to inhibit the heat shock response. IBT21 is useful for research related to prion diseases .
Art. -Nr.: HY-W097625R
CAS. Nr.: 26964-24-9
Art. -Nr.: HY-123996
CAS. Nr.: 20041-64-9
Forschungsgebiete:
3-Ethoxy-5,6-dibromosalicylaldehyde is an IRE1/ERN1 inhibitor, with an IC50 of 0.12 μM, a Ki of 71-88 nM, and a Kd of 100 nM against the ribonuclease activity of hIRE1α, as well as an IC50 of 4.8 μM against yeast Ire1. It shows selectivity toward IRE1 ribonuclease. 3-Ethoxy-5,6-dibromosalicylaldehyde blocks the IRE1/ERN1-mediated unfolded protein response (UPR) signaling pathway, including XBP-1 mRNA splicing, induction of XBP1 target genes, and activation of MAPK8/9/10, but does not alter the phosphorylation level of IRE1α or the PERK/ATF6 pathway. 3-Ethoxy-5,6-dibromosalicylaldehyde inhibits chikungunya virus replication, induces growth arrest, apoptosis and clonogenic inhibition in pancreatic cancer cells, reduces FB1 (Fumonisin B1) (HY-N6719)-induced autophagy and cell death, regulates PGG-induced senescence and apoptosis, and alleviates Sorafenib (HY-10201)-induced vacuolization and damage in hepatic stellate cells. 3-Ethoxy-5,6-dibromosalicylaldehyde can be used in research related to chikungunya virus infection, pancreatic cancer, FB1-induced nephrotoxicity, liver cancer, breast cancer, lung cancer and liver fibrosis .
Art. -Nr.: HY-187519
KRAS-IN-61 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC50 <10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-61 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells. KRAS-IN-61 can inhibit tumor growth in vivo. KRAS-IN-61 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer .
Art. -Nr.: HY-187520
CAS. Nr.: 3137385-11-3
KRAS-IN-62 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC50 < 10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-62 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells (pERK IC90 = 0.51 nM in GP2D cells). KRAS-IN-62 inhibits tumor growth in vivo, with plasma concentrations exceeding IC50 for ~20 h after oral administration in beagle dogs. KRAS-IN-62 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer .
- 1
-
-
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
