Search Result
Results for "
p38α kinase
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-10295
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SB 202190
Maximum Cited Publications
134 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-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-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-10456
-
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p38 MAPK
Casein Kinase
Wnt
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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-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-107597
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Halicin
2 Publications Verification
SU3327
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JNK
|
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-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-111820
-
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Casein Kinase
p38 MAPK
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Cardiovascular Disease
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CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis .
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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-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-16715
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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-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-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-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-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-114221
-
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UR13870
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p38 MAPK
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Inflammation/Immunology
|
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Org 48762-0 (UR13870) is a potent, orally active and selective p38 inhibitor with an EC50 of 0.1 μM for p38α kinase. Org 48762-0 shows a high degree of kinase selectivity for p38α and p38β over other kinases. Org 48762-0 reduces Lipopolysaccharides (HY-D1056) (LPS)-induced TNFα release. Org 48762-0 can be used for the study of rheumatoid arthritis (RA) and Werner syndrome .
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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-139553A
-
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(R)-ATI-450; (R)-CDD-450
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Drug Isomer
|
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-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-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-119298
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p38 MAPK
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Inflammation/Immunology
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AW-814141 is a selective and orally active p38 MAP kinase inhibitor. AW-814141 has an IC50 values of 100 nM and 158 nM for p38-α and β isoforms, respectively. AW-814141 can inhibit the production of TNF-α induced by LPS (HY-D1056). AW-814141 can inhibit paw edema in rats in a dose-dependent manner. AW-814141 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases such as rheumatoid arthritis .
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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-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-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-105997
-
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p38 MAPK
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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-171279
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p38 MAPK
Casein Kinase
Apoptosis
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Inflammation/Immunology
|
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Casein kinase 1δ-IN-29 (Compound 18) is the inhibitor for p38α and casein kinase 1 that inhibits p38α, CK1δ and CK1ε with IC50 of 0.041 µM, 0.005 µM and 0.447 µM, respectively. Casein kinase 1δ-IN-29 arrests cell cycle at subG1 phase, induces apoptosis in cell AC1-M88 .
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- HY-171295
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p38 MAPK
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Inflammation/Immunology
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p38 Kinase inhibitor 7 (Comp:XXXIX) is the inhibitor for p38α with an IC50 of 5.25 nM. p38 Kinase inhibitor 7 inhibits TNFα production in cell THP-1 with an IC50 of 5.88 nM .
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- HY-171290
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Casein Kinase
p38 MAPK
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Inflammation/Immunology
|
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Casein kinase 1δ-IN-31 (Compound 16) is the inhibitor for casein kinase (CK) that inhibits CK1α, CK1δ, and p38α with IC50s of 196, 17, and 18 nM, respectively. Casein kinase 1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with IC50 of 1200 nM .
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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-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-171277
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Casein Kinase
p38 MAPK
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Cancer
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Casein kinase 1δ-IN-27 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1α, CK1δ, CK1ε, and p38α with IC50s of 22, 16.5, 9.41 and 14.8 nM, respectively. Casein kinase 1δ-IN-27 inhibits the DUX4 expression with an IC50 of 10 nM .
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- HY-10441
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p38 MAPK
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Cancer
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BMS-626531 is a potent and selective p38α MAP kinase inhibitor. BMS-626531 can be used for the research of cancer .
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- HY-175432
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p38 MAPK
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Inflammation/Immunology
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p38 MAPK-IN-9 (Compound 15) is an orally active and highly selective p38α mitogen-activated protein kinase (p38 MAPK) inhibitor with an IC50 value of 9.6 nM. p38 MAPK-IN-9 is promising for research of inflammatory diseases such as rheumatoid arthritis, septic shock, and chronic obstructive pulmonary disease (COPD) .
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- HY-10295AR
-
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Organoid
Reference Standards
p38 MAPK
Autophagy
Apoptosis
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Neurological Disease
Cancer
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SB 202190 (hydrochloride) (Standard) is the analytical standard of SB 202190 (hydrochloride). This product is intended for research and analytical applications. 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-10320R
-
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BIRB 796 (Standard)
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Reference Standards
p38 MAPK
Raf
Autophagy
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Inflammation/Immunology
Cancer
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Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. 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-10295R
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Organoid
Reference Standards
p38 MAPK
Autophagy
Apoptosis
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Neurological Disease
Cancer
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SB 202190 (Standard) is the analytical standard of SB 202190. This product is intended for research and analytical applications. 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-171292
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Casein Kinase
p38 MAPK
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Others
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CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC50 of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC50 of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance .
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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-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-183531
-
|
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p38 MAPK
|
Inflammation/Immunology
|
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p38 MAP Kinase-IN-4 is a p38α MAPK inhibitor with an IC50 of 40.5 nM. p38 MAP Kinase-IN-4 is applicable to inflammation-related research .
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- HY-18758R
-
|
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TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
IN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. 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-125500
-
|
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p38 MAPK
Syk
Src
|
Neurological Disease
|
|
TOP1362 is a narrow spectrum kinase inhibitor. TOP1362 is a potent inhibitor of P38-α and Syk kinases with Kd values of 26 and 18 nM, respectively and an IC50 of 14 nM in the Src kinase activity assay. TOP1362 potently inhibits P38-α, Src and Syk. TOP1362 can be used in the research of dry eye syndrome .
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- HY-107597R
-
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SU3327 (Standard)
|
Reference Standards
JNK
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Metabolic Disease
Inflammation/Immunology
|
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Halicin (Standard) is the analytical standard of Halicin (HY-107597). This product is intended for research and analytical applications. 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-18794
-
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p38 MAPK
TNF Receptor
Interleukin Related
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Inflammation/Immunology
|
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R-03201195 is an efficient and selective p38 MAP kinase inhibitor with an IC50 for p38α of 0.7 nM. R-03201195 has inhibitory activity against TNF-α in THP-1 cells and against IL-1β in human whole blood, with IC50 values of 0.25 and 0.57 nM respectively. R-03201195 can be used for inflammatory diseases such as rheumatoid arthritis .
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- HY-10456R
-
|
|
Reference Standards
p38 MAPK
Casein Kinase
Wnt
|
Inflammation/Immunology
|
|
TAK-715 (Standard) is the analytical standard of TAK-715 (HY-10456). This product is intended for research and analytical applications. 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-108642BR
-
|
|
Reference Standards
p38 MAPK
Casein Kinase
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Inflammation/Immunology
|
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AMG-548 dihydrochloride (Standard) is the analytical standard of AMG-548 (dihydrochloride) (HY-108642B). This product is intended for research and analytical applications. 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-121293
-
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p38 MAPK
|
Inflammation/Immunology
|
|
CP-944629 (Compound 20) is an inhibitor of p38 alpha kinase with an IC50 of 3.2. CP-944629 can be studied in research for chronic inflammation diseases .
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- HY-181139
-
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Anaplastic lymphoma kinase (ALK)
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Metabolic Disease
|
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ALK5-IN-86 (Compound 22f) is a selective ALK5 inhibitor with an IC50 of 0.267 μM. ALK5-IN-86 forms hydrogen bonds with key amino acid residues in the active site of ALK5. ALK5-IN-86 is applicable to the research of diseases such as liver fibrosis .
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- HY-18909
-
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Src
Bcr-Abl
Pyk2
p38 MAPK
c-Kit
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Others
|
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Multi-kinase-IN-11 (Compound 1a) is a DFG-out conformation-targeted multi-kinase inhibitor, including SRC, LCK, ABL, PYK2, CSK, HCK, P38 and C-KIT. Multi-kinase-IN-11 serves as a scaffold for the preparation of fluorescently labeled binding probes and affinity matrices .
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- HY-W015445R
-
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Reference Standards
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-119138
-
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p38 MAPK
MMP
PGE synthase
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Inflammation/Immunology
|
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R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression. R-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis .
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- HY-183042
-
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p38 MAPK
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Cancer
|
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p38α-IN-12 is an orally bioavailable p38α MAPK inhibitor, with an IC50 of 0.11 nM and a Ki of 0.2 nM against human targets. p38α-IN-12 inhibits the production of TNFα in cellular systems and exerts in vivo efficacy in acute mouse models .
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| Cat. No. |
Product Name |
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Classification |
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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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