MAP3K6 Inhibitors
Chemical inhibitors of MAP3K6 can act through various points within the MAPK signaling cascade to achieve functional inhibition. SP600125, a known JNK inhibitor, targets a downstream kinase in the MAPK pathway that MAP3K6 feeds into. By inhibiting JNK, SP600125 effectively disrupts the signaling relay that would normally result from MAP3K6 activation, leading to a cessation of downstream effects that MAP3K6 would typically promote. Similarly, PD98059 and U0126 are inhibitors of MEK, another kinase that operates downstream of MAP3K6. These compounds prevent MEK from activating ERK, which is a key player in the MAPK pathway. This interruption in the signaling cascade results in an indirect functional inhibition of MAP3K6, as the pathway's flow is hindered, preventing MAP3K6 from exerting its normal biological effects.
Further along the lines of indirect inhibition, compounds like SB203580, BIRB 796, and LY2228820 target p38 MAP kinase, disrupting the signaling pathway at a point downstream of MAP3K6. By preventing p38 MAPK's activity, these inhibitors negate the influence of MAP3K6 in stress response and cytokine production. Kinase inhibitors with broader spectra, such as Sorafenib, Sunitinib, Dasatinib, Gefitinib, Erlotinib, and Lapatinib, can functionally inhibit MAP3K6 by targeting other kinases and receptors that are either part of or interact with the MAPK pathway. For instance, Sorafenib's activity against Raf kinases and Sunitinib's impact on receptor tyrosine kinases can result in a decrease in MAP3K6 activity due to the fact that these kinases are upstream regulators of the MAPK pathway. Dasatinib's inhibition of Src family kinases, and the EGFR inhibition by Gefitinib, Erlotinib, and Lapatinib, all lead to a dampening of the signaling that would normally activate MAP3K6, thereby functionally inhibiting the protein by preventing its usual cellular response.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an anthrapyrazolone inhibitor known to inhibit c-Jun N-terminal kinase (JNK), which is a downstream target in the MAPK signaling pathway. MAP3K6 is an upstream activator of the JNK pathway; hence, inhibiting JNK with SP600125 can lead to the functional inhibition of MAP3K6 signaling output by preventing downstream signal propagation. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 is a synthetic molecule that inhibits mitogen-activated protein kinase kinase (MEK), which is part of the MAPK/ERK pathway. Although MAP3K6 is not directly in the ERK pathway, the inhibition of MEK with PD98059 can reduce the cross-talk between MAPK pathways and potentially diminish MAP3K6 mediated signaling through inhibitory regulatory loops. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is a non-competitive inhibitor of MEK1/2, which are downstream of MAP3K6 in the signaling cascade. By inhibiting MEK, U0126 can functionally inhibit the activity of MAP3K6 by preventing the activation of downstream effectors in the MAPK pathway. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a pyridinyl imidazole compound that selectively inhibits p38 MAP kinase, another downstream effector in the MAPK signaling pathway. Inhibition of p38 MAP kinase can lead to functional inhibition of MAP3K6 by disrupting the signaling pathways that are activated by MAP3K6. | ||||||
Doramapimod | 285983-48-4 | sc-300502 sc-300502A sc-300502B | 25 mg 50 mg 100 mg | $149.00 $281.00 $459.00 | 2 | |
BIRB 796 is a diaryl urea compound that inhibits p38α and p38β MAP kinases. By targeting these kinases, BIRB 796 can impede the signaling cascade initiated by MAP3K6, thus functionally inhibiting MAP3K6's role in cellular processes that depend on p38 MAPK signaling. | ||||||
LY2228820 | 862507-23-1 | sc-364525 | 5 mg | $191.00 | 1 | |
LY2228820 is a potent and selective inhibitor of p38 MAPK. By inhibiting p38 MAPK, LY2228820 can functionally inhibit MAP3K6 activity by blocking downstream signaling, thereby disrupting the cellular responses mediated by MAP3K6. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $56.00 $260.00 $416.00 | 129 | |
Sorafenib is a kinase inhibitor with activity against Raf kinases. While its primary targets are not in the MAP3K6 pathway, its broad kinase inhibition profile can lead to the inhibition of kinases within the MAPK pathways and consequently the functional inhibition of MAP3K6. | ||||||
Sunitinib, Free Base | 557795-19-4 | sc-396319 sc-396319A | 500 mg 5 g | $150.00 $920.00 | 5 | |
Sunitinib is a receptor tyrosine kinase inhibitor that, among others, can inhibit signaling pathways upstream of MAPK signaling. Although not directly inhibiting MAP3K6, Sunitinib can reduce the activation of MAP3K6 by inhibiting upstream kinases and growth factor signaling. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Dasatinib is a broad-spectrum tyrosine kinase inhibitor with potential to inhibit Src family kinases that interact with MAPK pathways. By inhibiting these kinases, Dasatinib can indirectly lead to the functional inhibition of MAP3K6 by impeding the activation of downstream signaling components. | ||||||
Gefitinib | 184475-35-2 | sc-202166 sc-202166A sc-202166B sc-202166C | 100 mg 250 mg 1 g 5 g | $62.00 $112.00 $214.00 $342.00 | 74 | |
Gefitinib is an EGFR inhibitor that can indirectly inhibit MAP3K6 by inhibiting EGFR-mediated activation of the MAPK signaling cascade, which includes MAP3K6 as a component. | ||||||