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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
45 Results for "
MK2
" in MedChemExpress (MCE) Product Catalog:
Products (45)
45 Results for "MK2" in MCE Product Catalog:
17
17 Publications Verification
Synonyms: LY2228820 dimesylate
Research Areas:
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
17
Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma [2].
6
6 Cited Publications
Target:
Research Areas:
MK2-IN-1 hydrochloride (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein [2].
6
6 Cited Publications
Target:
Research Areas:
MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein [2].
5
5 Cited Publications
Target:
Research Areas:
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo .
5
5 Cited Publications
Target:
Research Areas:
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 8.5 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2 .
2
2 Cited Publications
Target:
Research Areas:
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
1
1 Cited Publications
Cat. No.: HY-P10072A
Synonyms: Hsp25 kinase inhibitor acetate; MK2 pseudosubstrate acetate
Synonyms: ATI-450; CDD-450
Target:
Research Areas:
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .
Synonyms: MW01-18-150SRM
Research Areas:
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
Synonyms: CC-99677
Target:
Research Areas:
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
Cat. No.: HY-P3412
CAS No.: 1039342-24-9
Synonyms: MK2i peptide; YARA-MK2i
Target:
Research Areas:
Target:
Research Areas:
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330 nM [2].
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
Cat. No.: HY-P10072
CAS No.: 474713-20-7
Synonyms: Hsp25 kinase inhibitor; MK2 pseudosubstrate
Cat. No.: HY-179237
Target:
Research Areas:
MK2-IN-8 (Compound 42) is a covalent MK2 kinase inhibitor. MK2-IN-8 forms a unique covalent bond with the catalytic lysine, thereby demonstrating that the fluorosulfonate can effectively target the catalytic lysine in kinases.
Cat. No.: HY-172807
CAS No.: 2133007-20-0
Target:
Research Areas:
p38α-IN-9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC50 lower than 20 nM. p38α-IN-9 inhibits MK2 T334 phosphorylation. p38α-IN-9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α-IN-9 Inhibits colorectal cancer (CRC) metastasis .
Cat. No.: HY-162700
Target:
Research Areas:
MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer .
Cat. No.: HY-W726640
CAS No.: 35265-50-0
Target:
Research Areas:
Peraquinsin is a MK2 activator. Peraquinsin can be used for the research of vascular disorder or endothelial barrier disorder. Peraquinsin also is an antihypertensive agent .
Cat. No.: HY-147283
CAS No.: 1105658-32-9
Target:
Research Areas:
MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor with an IC50 value of 45 nM. MK2-IN-4 can be used in the research of cancer, inflammation, immunology .
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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
