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.

MARK Inhibitors (8)

MARK Related Products (10):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-120877

MRT199665	Inhibitor	99.74%
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.

HY-139604

PCC0208017	Inhibitor	98.03%
PCC0208017 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.

HY-114317

MARK4 inhibitor 1	Inhibitor	98.29%
MARK4 inhibitor 1 is a potent and selective microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC₅₀ of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.

HY-112266

MARK-IN-4	Inhibitor	98.99%
MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC₅₀ of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease.

HY-101934

MARK-IN-2	Inhibitor	99.19%
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC₅₀ of 5 nM.

HY-120877A

(R)-MRT199665	Inhibitor	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.

HY-159113

PCC0105003	Inhibitor
PCC0105003 is a potent MARK inhibitor. PCC0105003 can be used in the study of neuropathic pain.

HY-154988

MARK4 inhibitor 4		99.23%
MARK4 inhibitor 4 is a MARK4 inhibitor with an IC₅₀ of 1.49 μM. MARK4 inhibitor 4 can be used in cancer and tau lesion-related research.

HY-154986

MARK4 inhibitor 2	Inhibitor	99.47%
MARK4 inhibitor 2 is an inhibitor of microtubule affinity-regulating kinase 4 (MARK4) with an K_m of 6.3×10 ⁷ and an IC₅₀ of 0.82 μM. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research.

HY-154987

MARK4 inhibitor 3		98.23%
MAPK4 inhibitor 3 (compound 23b) is an inhibitor of MAPK4 with an IC₅₀ value of 1.01 μM. MAPK4 inhibitor 3 inhibits cancer cells growth. MAPK4 inhibitor 3 can be used for research on cancer and tauopathies.

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