MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, modulate many biological processes, such as growth, development and various environmental stresses. Based on the sequence of their kinase catalytic domain, MAP3Ks are classified into three groups: the MEKK-like, ZIK-like and Raf-like families. Raf-like MAP3Ks constitute largest MAP3K subfamily. Raf-like MAP3Ks play roles in response to biotic and abiotic stresses.
MAP3Ks often bind to both MAP4Ks and MAP2Ks in the same pathway. For example, MEKK1 (MAP3K1) binds to both the MAP4K NIK and the MAP2K MKK4, while NSY-1 (MAP3K) binds to the MAP2K SEK-1. MAP3Ks activates MAP2Ks by phosphorylation of a serine and/or threonine, and MAP2Ks activate MAPKs by dual phosphorylation of a Thr-X-Tyr motif.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H8957 |
GNE-8505 |
1620573-48-9 | GNE-8505 is a novel, potent and orally bioavailable inhibitor of Dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 4 nM. |
H7399 |
TCASK10 |
1005775-56-3 | TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM, 30-fold selectivity over ASK2 (IC50=510 nM) and no activity against MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf; blocks downstream JNK1/p38 phosphorylation in cells, dose-dependently reduces mitogen (FBS, PDGF and EGF)-induced airway smooth muscle (ASM) growth, also prevents TGFb1-induced migration of ASM cells in vitro. |
H7398 |
TAOK inhibitor 63 |
850467-91-3 | TAOK inhibitor 63 is a novel potent, selective, ATP-competitive TAO Kinase (TAOK) inhibitor with IC50 of 19 and 39 nM against TAOK1 (MAP3K16) and TAOK2 (MAP3K17), respectively; increases the mitotic population, the percentages of mitotic cells displaying amplified centrosomes and multipolar spindles, induces cell death, and inhibits cell growth in centrosome-amplified SKBR3 or BT549 breast cancer cell models. |
H7397 |
TAOK inhibitor 43 |
850467-66-2 | TAOK inhibitor 43 is a novel potent, selective, ATP-competitive TAO Kinase (TAOK) inhibitor with IC50 of 11 and 15 nM against TAOK1 and TAOK2, respectively; increases the mitotic population, the percentages of mitotic cells displaying amplified centrosomes and multipolar spindles, induces cell death, and inhibits cell growth in centrosome-amplified SKBR3 or BT549 breast cancer cell models. |
H7396 |
SW-083688 |
422281-45-6 |
SW-083688 (SW083688) is a potent, highly selective TAOK2 (Thousand-And-One Kinase 2, MAP3K17) inhibitor with IC50 of 1.3 uM; increases the abundance of p62 and inhibits autophagy; TAOK2 is an activator of p38 MAP kinase cascade that is up-regulated in response to environmental stresses, and a potential cancer therapeutic target. |
H7395 |
SW-034538 |
412919-82-5 | SW-034538 is a potent TAOK2 (Thousand-And-One Kinase 2; MAP3K17) inhibitor with IC50 of 300 nM, has cross-reactivity with respect to six of the 45 kinases (Raf1, GSK3β, JNK1, IRAK4, HGK and CDK2). |
H7394 |
Selonsertib |
1448428-04-3 |
Selonsertib (GS-4997)?is a highly selective and potent, ATP-competetive inhibitor of ASK1 (Apoptosis Signal-regulating Kinase 1,?MAP3K5) with potential anti-inflammatory, antineoplastic and anti-fibrotic activities; orally bioavailable. |
H7393 |
NQDI-1 |
175026-96-7 | NQDI-1 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with Ki of 500 nM; inhibits in vivo expression levels of ASK1, phosphorylated (p‑)JNK, p‑c‑Jun, p53 and caspase 3 in Hypoxia-ischemia rat model; enhances endochondral bone formation by increasing chondrocyte survival in mice. |
H7392 |
MEKK2 inhibitor 1s |
2412882-95-0 | MEKK2 inhibitor 1s (MEKK2-IN-1s) is a potent MEKK2 (MAP3K2) inhibitor with IC50 of 16 nM, inhibits MEKK2 and MEKK3 with similar potencies; displays activity in cell-based assays in which it inhibited ERK5 pathway activation in cells and inhibited cell migration in a scratch assay. |
H7391 |
MAP3K14-IN-173 |
2113617-02-8 | A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation); inhibits p-IKKα levels of L363 (NIK translocated multiple myeloma) cells with IC50 of 1.3 nM; exhibits antiproliferative activity on JJN-3 (NIK translocated) multiple myeloma cells (IC50=29 nM). |
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