p38

p38α inhibitor 4 is a selective MAPK p38α inhibitor, which is used to study diabetes, pain and chronic inflammation.

p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase (IC50 = 35 nM). It inhibits senescence induced by the oncogene RAS.

PLK1/p38γ-IN-1 (compound 14) serves as a dual inhibitor targeting both PLK1 and p38γ kinases, effectively suppressing the proliferation of human hepatocellular carcinoma and hepatoblastoma cell lines in vitro [1].

p38α inhibitor 3 is a inhibitor of the mitogen-activated protein kinase p38α that can block the effectiveness of myoblast differentiation.

p38 MAPK-IN-2 is an inhibitor of p38 kinase.

p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, displaying antitumor properties by promoting apoptosis and increasing reactive oxygen species (ROS) production [1].

p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.

p38 MAPK-IN-1 displays sustained levels, low clearance, and good bioavailability. p38 MAPK-IN-1 is a novel effective and selective inhibitor of p38 MAPK (IC50: 68 nM).

P38-α MAPK-IN-5 is a potent inhibitor of p38α, demonstrating inhibitory concentrations (IC50) of 0.1 nM for p38α, 0.2 nM for p38β, 944 nM for p38γ, and 4100 nM for p38δ. It exhibits anti-inflammatory properties and holds potential for research in asthma and chronic obstructive pulmonary disease (COPD).

p38-α MAPK-IN-1 is a MAPK14 (p38-α) inhibitor(IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay).

p38-α MAPK-IN-4 (Compound 69) is a selective inhibitor of p38α MAPK, demonstrating potent inhibition with an IC50 of 1.5 μM. It effectively and swiftly mitigates the onset of mechanical allodynia (MA) in vivo [1].

p38 MAP Kinase Inhibitor Ⅵ is a potent p38 MAP Kinase inhibitor with anti-inflammatory activity.

Compound 135, also known as p38 Kinase Inhibitor 4, is a potent inhibitor of p38 [1].

TOPK-p38/JNK-IN-1 (Compound B12) is an orally active inhibitor of the TOPK-p38/JNK signaling pathway, with an IC50 value of 2.14 μM for the inhibition of NO production. It demonstrates anti-inflammatory properties by inhibiting downstream phosphorylation of related proteins and preventing the degradation of TOPK [1].

(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively).

P38α Inhibitor 2, a potent and selective inhibitor of p38α MAPK, exhibits a pIC50 value of 9.6. It also demonstrates inhibition of the hERG ion channel (IC50=27 μM) and maintains promising selectivity, with <30% inhibition across a panel of 51 protein kinases at a 10 μM concentration and a broad specificity against 141 other biological targets[1].

Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.

LXH254 is a potent C-Raf and B-Raf inhibitor.

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.

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.

Dihydrocaffeic acid is a metabolite of chlorogenic acid, a well-known antioxidant component with antioxidant, anti-Alzheimer's disease, neuroprotective, arousal and lipid-lowering effects.

1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act

UR-13870 (Org 48762-0) is an orally active and selective inhibitor of p38 mitogen-activated protein kinase (MAPK), which prevents bone damage in collagen-induced arthritis in mice.

Iroxanadine (BRX-005) is a Novel small molecule MAPK p38 inhibitor that induces phosphorylation of p38 SAPK and induces concentration-dependent relaxation in guinea pig pulmonary artery preparations precontracted with phenylephrine.CAS 번호13480-84-5

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.

L-797,591 hydrochloride is active for somatostatin receptor isoform 1 (SSTR1). L-797,591 hydrochloride is commonly used in combination with AG1478 to enhance p-ERK5 expression in SSTR1 cells. L-797,591 hydrochloride significantly enhanced p38 phosphorylation in cotransfected cells, and this effect was reversed in combination with AG1478.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Apelin-12 acetate possesses a high affinity to orphan receptor APJ receptor. Apelin-12 acetate inhibits the JNK and p38 MAPK signaling pathway of the apoptosis-related MAPKs family, thus offering protection to neurons.

EO-1606 is a p38MAP kinase inhibitor with anti-inflammatory activity and may be used in studies of Alzheimer;s disease and dermatitis.

DIPQUO hydrochloride is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO hydrochloride promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.

JIP-1 (153-163) acetate(438567-88-5 free base) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). JIP-1 (153-163) acetate(438567-88-5 free base) binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.

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.

JNJ-49095397 (RV568) is a selective p38 MAPK-α and p38 MAPK--γ kinase inhibitor with anti-inflammatory activity and potential antiviral activity for chronic obstructive pulmonary disease (COPD), cystic fibrosis, and respiratory syncytial virus infection.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

AL 8697 is a selective p38α MAPK inhibitor (IC50 = 6 nM) with 14-fold selectivity over p38β (IC50 = 82 nM) and 300-fold selectivity over a panel of 91 kinases. AL 8697 has anti-inflammatory activity.

Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide indirectly decreases osteoclast differentiation through a decreased RANKL/OPG ratio. Muramyl dipeptide directly increases osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide is an inducer of bone formation through the induction of Runx2 .

Talmapimod (SCIO-469) is an selective, orally active, and ATP-competitive p38α inhibitor with IC50 of 9 nM and 90 nM for p38α and p38β, respectively. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

SR-318 is a potent and highly selective inhibitor of p38 MAPK(IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively), has anti-cancer and anti-inflammatory activity.

SHP389 is an allosteric SHP2 inhibitor, with an IC 50 of 36 nM for both SHP2 and p-ERK.

EXP3892 is an angiotensin II receptor antagonist.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

TAK-715 is a p38 MAPK inhibitor for p38α.

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.

Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.

BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).