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MAPKMAP3K
MAP3K (Mitogen Activated Protein (MAP) kinase kinase kinase) is a serine/threonine-specific protein kinase that acts on MAP kinases and belongs to the upstream component of the MAPK signaling pathway.Most of the MAP3Ks are activated by GPCR, stress, or growth factors, and then regulate the next level of the MAP2K and cascade reactions, which ultimately affect cell proliferation, differentiation, apoptosis and stress, and are implicated in cancer, inflammation and neurodegenerative diseases.
PF-05381941
T360171474022-02-0
PF-05381941 is a selective and potent dual inhibitor of TAK1 and p38α with IC 50 =156 nM 186nM that inhibits the kinase activity of TAK1 by binding to its active site.
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TAK-756
T204351
TAK-756 is a TAK1 inhibitor that selectively targets IRAK1 4 and exhibits excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) due to its complementary anti-catabolic and anti-inflammatory effects.
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Triptriolide
TN10461137131-18-1
Triptriolide inhibits puromycin aminonucleoside (PAN)-induced apoptosis in mouse podocytes by modulating Bcl-2 family proteins and suppressing Caspase-3. It also promotes cell survival and protects podocyte function by activating the TAK1-NF-κB signaling pathway and upregulating the podocyte protein podocin.
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KAI-11101
T204384
KAI-11101 is an inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. It effectively suppresses paclitaxel-induced cJun phosphorylation (IC50=95 nM), thereby inhibiting the activation of the MAPK pathway. KAI-11101 exhibits blood-brain barrier permeability, allowing for further exploration of its neuroprotective properties.
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PROTAC LZK-IN-1
T2043732763268-64-8
PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. This compound is applicable in anticancer research.
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Anti-inflammatory agent 102
T2071683053104-47-2
Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).
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CBP-501 acetate
TP3244
CBP-501 acetate is a cell-permeable calmodulin-binding peptide and a candidate G2 phase checkpoint abrogator. It inhibits several Ser216-specific kinases, including MAPKAP-K2, C-Tak1, CHK1, and CHK2, with IC50 values of 0.9 μM, 1.4 μM, 3.4 μM, and 6.5 μM, respectively. CBP-501 acetate is applicable to various cancer research studies.
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