MARK
Microtubule affinity regulating kinase
Microtubule affinity-regulating kinases belong to the calcium/calmodulin-dependent protein kinase superfamily. MARKs and their homologs are functionally diverse protein kinases, possessing functional roles in cell polarity, microtubule stability, cell cycle control and intracellular signaling. Phosphorylation of the catalytic kinase domain (KD) by upstream kinases like MARKK (MARK kinase) can lead to activation of MARK. Activated MARK can phosphorylate tau protein and other related MAP proteins such as MAP2 and MAP4, which have affinities for stabilizing microtubules, and also can phosphorylate other proteins involved in cell signaling and 14-3-3 (also known as Par 5, partitioning defective protein 5) binding.
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MARK Related Products (14)
Related Products (14)
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PCC0208017
0 ImagesPCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
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MRT199665
0 ImagesMRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
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MARK-IN-4
0 ImagesMARK-IN-4 (Compound 18) is a MARK inhibitor with an IC50 of 1 nM. MARK-IN-4 is applicable to Alzheimer's disease research.
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OICR19451
0 ImagesCat. No.: HY-182743CAS No.: 2803349-61-1OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer.
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(R)-MRT199665
0 ImagesCat. No.: HY-120877APurity: 98.70%(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
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PDK1-IN-1
0 ImagesPDK1-IN-1 (Compound 2-11) is a PDK1 inhibitor. PDK1-IN-1 is also useful as inhibitor of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. PDK1-IN-1 selectively inhibits microtubule affinity regulating kinase (MARK). PDK1-IN-1 can be used for researches of myeloproliferative disorders, cancer and Alzheimer's disease.
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MARK-IN-2 (Standard)
0 ImagesCat. No.: HY-101934RCAS No.: 1314893-26-9
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Kukoamine B mesylate
0 ImagesCat. No.: HY-N2393ACAS No.: 1375179-86-4Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis. .
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