Search Result
Results for "
p38α inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114423
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- HY-153002
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- HY-131335
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p38 MAPK
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Inflammation/Immunology
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p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
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- HY-159799
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p38 MAPK
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Cancer
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p38α inhibitor 5 (compound 1) is a PROTAC-type target protein ligand targeting p38 and can be used to synthesize NR-11c (HY-159798) .
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- HY-18874
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p38 MAPK
Autophagy
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Others
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p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay .
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- HY-14412
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p38 MAPK
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Cancer
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p38α inhibitor 4 (compound 10) is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM. p38α inhibitor 4 exhibits no activity against p38β, p38γ, and p38δ .
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- HY-161293
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p38 MAPK
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Cancer
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p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
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- HY-146032
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- HY-162364
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p38 MAPK
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Neurological Disease
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p38-α MAPK-IN-7 (compound 4) is a p38α-MAPK inhibitor with an IC50 value of 98.7 nM. p38-α MAPK-IN-7 protects neuronal cells from dexamethasone-induced ROS production .
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- HY-147518
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p38 MAPK
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Inflammation/Immunology
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p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research .
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- HY-161462
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ERK
p38 MAPK
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Cancer
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ERK2/p38α MAPK-IN-1 (Compound 1, In silico Hit-2) is a potent and selective ERK2 and p38α MAPK inhibitor, with an IC50 of 82 μM for ERK2. ERK2/p38α MAPK-IN-1 binds to the allosteric site of ERK2 and p38α MAPK in distinct manners. ERK2/p38α MAPK-IN-1 can be used for the research of type 2 diabetes .
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- HY-14975
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p38 MAPK
Autophagy
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Cancer
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R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively .
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- HY-10401
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- HY-168841
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- HY-11087
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SD-06
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p38 MAPK
Autophagy
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Inflammation/Immunology
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SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α .
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- HY-108645
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p38 MAPK
Autophagy
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Inflammation/Immunology
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AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .
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- HY-112401
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p38 MAPK
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Inflammation/Immunology
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p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
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- HY-10328
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VX-745
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p38 MAPK
Autophagy
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Inflammation/Immunology
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Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
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- HY-105997
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Others
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Others
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AZD 6703 is a p38α MAP kinase inhibitor with activity in inflammatory diseases.
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- HY-14305
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p38 MAPK
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Inflammation/Immunology
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BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
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- HY-10403
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- HY-120111
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MW01-18-150SRM
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p38 MAPK
Autophagy
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-120823
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- HY-N8251
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- HY-159798
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PROTACs
p38 MAPK
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Cancer
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NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)) .
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- HY-151921
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p38 MAPK
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Inflammation/Immunology
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Anti-inflammatory agent 33 is a potent p38α inhibitor. Anti-inflammatory agent 33 inhibits NO production. Anti-inflammatory agent 33 inhibits LPS-induced iNOS, COX-2, p-p38α, p-MK2 protein expression. Anti-inflammatory agent 33 shows anti-inflammatory activity .
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- HY-120111A
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MW01-18-150SRM hydrochloride
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p38 MAPK
Autophagy
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Neurological Disease
Inflammation/Immunology
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MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
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- HY-16715
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- HY-120111B
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MW01-18-150SRM dihydrochloride dihydrate
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p38 MAPK
Autophagy
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Neurological Disease
Inflammation/Immunology
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MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
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- HY-135674
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p38 MAPK
TNF Receptor
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Inflammation/Immunology
Cancer
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SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
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- HY-11068
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p38 MAPK
Autophagy
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Inflammation/Immunology
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SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD .
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- HY-110398
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Baicalein trimethyl ether
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p38 MAPK
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Inflammation/Immunology
Cancer
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5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera .
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- HY-14974
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p38 MAPK
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Inflammation/Immunology
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R 1487 is an orally active and highly selective p38α mitogen-activated protein kinase inhibitor. R 1487 can be used in the study of rheumatoid arthritis .
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- HY-136794
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p38 MAPK
Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .
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- HY-145564A
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PF-07265803 hydrochloride
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p38 MAPK
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Cardiovascular Disease
Inflammation/Immunology
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Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
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- HY-112182
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DAS-DFGO-II
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Src
p38 MAPK
Autophagy
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Cancer
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UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
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- HY-10402
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- HY-12299
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Dual LCK/SRC inhibitor
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Src
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Cancer
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WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
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- HY-144697
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- HY-14305A
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p38 MAPK
Autophagy
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Inflammation/Immunology
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BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
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- HY-160930
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p38 MAPK
Src
Syk
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Inflammation/Immunology
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TOP1288 is a narrow spectrum kinase inhibitor for P38α, Src and Syk kinase, with IC50 of 116nM, 24nM and 659nM, respectively. TOP1288 inhibits inflammatory cytokine release from inflamed biopsies and myofibroblasts .
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- HY-139553
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ATI-450; CDD-450
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MAPKAPK2 (MK2)
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Inflammation/Immunology
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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 .
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- HY-108646
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p38 MAPK
JNK
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Inflammation/Immunology
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SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable .
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- HY-16782
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ARRY-614
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Tie
p38 MAPK
Autophagy
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Cancer
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Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
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- HY-107597
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Halicin
1 Publications Verification
SU3327
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JNK
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Metabolic Disease
Inflammation/Immunology
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Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
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- HY-W015445
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p38 MAPK
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Metabolic Disease
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SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
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- HY-18759
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p38 MAPK
TNF Receptor
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Inflammation/Immunology
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BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
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- HY-163429
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TGF-β Receptor
p38 MAPK
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Inflammation/Immunology
Cancer
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J-1149 is a potent ALK5 inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research .
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- HY-139553A
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(R)-ATI-450; (R)-CDD-450
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Drug Isomer
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Inflammation/Immunology
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(R)-Zunsemetinib is the isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. 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 .
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- HY-151233
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TGF-β Receptor
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Cancer
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ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer .
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- HY-145564
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PF-07265803
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p38 MAPK
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Cardiovascular Disease
Inflammation/Immunology
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Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
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- HY-10320
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BIRB 796
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p38 MAPK
Raf
Autophagy
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Inflammation/Immunology
Cancer
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Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM .
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- HY-10406
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SCIO-469
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p38 MAPK
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Cancer
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Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
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- HY-10406A
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SCIO-469 hydrochloride
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p38 MAPK
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Cancer
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Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs .
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- HY-15505
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JNJ 3026582
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p38 MAPK
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity .
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- HY-10295A
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Organoid
p38 MAPK
Autophagy
Apoptosis
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Neurological Disease
Cancer
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SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .
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- HY-10295
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SB 202190
Maximum Cited Publications
94 Publications Verification
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Organoid
p38 MAPK
Autophagy
Apoptosis
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Neurological Disease
Cancer
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SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .
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- HY-10405
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Ro4402257; R1503
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p38 MAPK
Autophagy
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Inflammation/Immunology
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Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
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- HY-18766
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TGF-β Receptor
p38 MAPK
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Cancer
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EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung .
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- HY-13241A
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LY2228820
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p38 MAPK
Autophagy
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Inflammation/Immunology
Cancer
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Ralimetinib (LY2228820) is a potent and 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 p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
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- HY-18303
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AMG-47a
3 Publications Verification
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Src
VEGFR
p38 MAPK
JAK
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Inflammation/Immunology
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AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity .
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- HY-10456
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
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- HY-18862
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p38 MAPK
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Inflammation/Immunology
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PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
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- HY-108642
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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- HY-108642B
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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- HY-108642A
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p38 MAPK
Casein Kinase
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Inflammation/Immunology
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AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
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- HY-18758
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IN-1130
1 Publications Verification
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TGF-β Receptor
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Inflammation/Immunology
Cancer
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IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
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- HY-10320G
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BIRB 796 (GMP)
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p38 MAPK
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Cancer
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Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
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- HY-10405S
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Isotope-Labeled Compounds
p38 MAPK
Autophagy
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Inflammation/Immunology
|
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
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- HY-125387
-
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Src
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Inflammation/Immunology
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TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
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- HY-108346
-
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p38 MAPK
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Inflammation/Immunology
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JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation .
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- HY-10403A
-
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p38 MAPK
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Inflammation/Immunology
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(aS)-PH-797804 is a selective p38 MAPK inhibitor with IC50 values for p38 α /β of 26 nM and 102 nM, respectively. (aS)-PH-797804 has anti-inflammatory activity .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-10405S
-
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Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
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Cat. No. |
Product Name |
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Classification |
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- HY-159799
-
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Alkynes
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p38α inhibitor 5 (compound 1) is a PROTAC-type target protein ligand targeting p38 and can be used to synthesize NR-11c (HY-159798) .
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- HY-125387
-
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Alkynes
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TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
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