MARK Inhibitor

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.

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.

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

MARK-IN-4 (Compound 18) is a MARK inhibitor with an IC₅₀ of 1 nM. MARK-IN-4 is applicable to Alzheimer's disease research.

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.

OICR19451 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.

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.

(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.

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

PDK1-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.

MARK-IN-2 (Standard) is the analytical standard of MARK-IN-2 (HY-101934). This product is intended for research and analytical applications. MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC₅₀ of 5 nM.

Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with K_d 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. .