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MAPKp38 MAPK
p38 MAPKs (α, β, γ, and δ) are members of the MAPK family that are activated by a variety of environmental stresses and inflammatory cytokines. As with other MAPK cascades, the membrane-proximal component is a MAPKKK, typically a MEKK or a mixed lineage kinase (MLK). The MAPKKK phosphorylates and activates MKK3/6, the p38 MAPK kinases. MKK3/6 can also be activated directly by ASK1, which is stimulated by apoptotic stimuli. p38 MAPK is involved in regulation of HSP27, MAPKAPK-2 (MK2), MAPKAPK-3 (MK3), and several transcription factors including ATF-2, Stat1, the Max/Myc complex, MEF-2, Elk-1, and indirectly CREB via activation of MSK1.
Darizmetinib
T729562369583-33-3
Darizmetinib (HRX215, HRX-0215) is an MKK4 inhibitor. Inhibition of MKK4 leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration.
- $155
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Afatinib
Cited
T21312850140-72-6
Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.
- $30
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CitedSB 202190 Cited
T2301152121-30-7
SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.
- $35
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CitedBilobetin
Cited
T4S2128521-32-4
Bilobetin ameliorates insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet.
- $39
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CitedCytochalasin D
T322922144-77-0
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
- $239
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Ergothioneine
T8191497-30-3
Ergothioneine (L-(+)-Ergothioneine) is synthesized by certain bacteria and fungi. It is generally considered an antioxidant.
- $31
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12(S)-HETE
T3704754397-83-0
12(S)-HETE, a 12-lipoxygenase metabolite of arachidonic acid, is mitogenic for cancer cell proliferation and enhances angiotensin II-induced contraction of BLT2 (type 2 receptor in arteries of leukotriene B4 mice) and TP (thromboxane receptor)-mediated mechanisms. 12(S)-HETE promotes superoxide and isothromboxane-like metabolites in arterial endothelial cells. production.
- $642
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Adezmapimod Cited
T1764152121-47-6
Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.
- $30
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Cited
T25015897644-83-6In house
AKP-001 is a selective inhibitor of MAPK of the p38α isoform and is used in the study of immune and digestive disorders.
- $293
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BI-3406 Cited
T129792230836-55-0
BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.
- $67
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CitedMadecassoside
T281334540-22-2
Madecassoside (Asiaticoside A) is a pentacyclic triterpene extracted from Centella asitica (L.) with anti-inflammatory, anti-oxidative and anti-aging activities.
- $44
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SU9516
T6167377090-84-1
SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
- $30
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LXH254 Cited
T118981800398-38-2
LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.
- $48
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CitedSSK1
T374502629250-69-5In house
SSK1 is a compound that selectively kills senescent cells and is a precursor for β-galactosidase, which can reduce the inflammatory response of the body. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, and promote mitochondrial DNA damage in senescent cells.
- $156
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Chrysoeriol Cited
TN1490491-71-4
Chrysoeriol has antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities, it also shows selective bronchodilator effect.
- $40
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CitedAsiaticoside
T302516830-15-2
Asiaticoside (Emdecassol) (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burns.
- $50
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MW-150
T54941628502-91-9
MW-150 (MW01-18-150SRM) is a unique, selective, CNS-penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
- $33
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Vincristine
T3S020957-22-7
Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and
- $34
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p38 mapk inhibitor
T36010219138-24-6In house
p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM). It inhibits senescence induced by the oncogene RAS.
- $54
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Butyzamide
T678941110767-45-7In house
Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.
- $285
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Solamargine
T403420311-51-7
Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.
- $54
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Exarafenib
T636442639957-39-2
Exarafenib (RAF KIN_2787) is a potent, orally available pan-RAF inhibitor with antitumor activity that acts by inhibiting downstream MAPK pathway signaling. It is used in cancer research.
- $131
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Hesperetin Cited
T2565520-33-2
Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.
- $38
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