mk2

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

MK2-IN-3 hydrate (MK-2 Inhibitor III) is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)

MK2-IN-1 hydrochloride (MK 25) is a highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2, IC50: 0.11 μM) [1].

MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis

MK2-IN-5, a pseudosubstrate of Mk2 with an inhibition constant (K_i) of 8 μM, selectively targets the protein interaction domain of the MAPK pathway and inhibits the phosphorylation of HSP25 and HSP27 [1] [2] [3].

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated

Zunsemetinib (ATI-450) is an orally active and selective inhibitor of the p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway.Zunsemetinib is used to study spondyloarthritis and rheumatoid arthritis.

CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM).

p38α-MK2-IN-1 (Compound 36) is an inhibitor of the p38α-MK2 complex, with an IC50 of 5 nM. This compound exhibits significant anti-inflammatory properties and has the ability to aid in joint repair.

MK2-IN-7 (Compound 144) is an inhibitor of mitogen-activated protein kinase-activated protein kinase-2 (MK2). It shows potential for research in inflammatory diseases, autoimmune disorders, and cancer.

MK2-IN-4, a MAPKAPK2 (MK2) inhibitor with an IC50 of 45 nM, can be used in cancer, inflammation, and immunology studies.

MK2-IN-6 (Compound 11) is an effective and selective irreversible inhibitor of MK2 with an IC50 value of 2.3 nM. It suppresses the kinase activity of MK2, leading to sustained inhibition of MK2 signaling and reduction of pathological inflammatory factors in macrophages. MK2-IN-6 is capable of inhibiting the M2-like protein phenotype in macrophages both in vitro and in vivo, showing potential for use in colorectal cancer research.

Adenosine 5'-methylenediphosphate (sodium salt) is also referred to as an inhibitor of ecto-5'-nucleotidase.

MK256 is a novel CDK8 inhibitor that demonstrates potent antitumor activity against AML by inhibiting the STAT pathway. It induces differentiation and maturation while inhibiting proliferation in AML cell lines. MK256 decreases the phosphorylation of STAT1(S727) and STAT5(S726) and reduces mRNA expression of MCL-1 and CCL2 in these cells. Its efficacy is validated in the MOLM-14 xenograft model, showing phosphorylation inhibition of STAT1(S727) and STAT5(S726) post-treatment. Pharmacokinetic studies in the MOLM-14 model reveal a dose-dependent inhibition of the STAT pathway. Both in vitro and in vivo studies confirm that MK256 effectively downregulates the STAT pathway.

MK204 is an inhibitor of AKR1B10, a tumor marker and promising antineoplastic target.

UR-MK299 is a NPY Y1 receptor antagonist.

AMK218 (Immobilized amoxicillin acylase) serves as a biocatalyst and is a key enzyme in new biocatalyst technologies. Enzyme engineering focuses on improving enzyme reaction kinetics, substrate selectivity, and activity under extreme conditions (e.g., low or high pH). Modifications that introduce stimulus responsiveness enable dynamic control of their activity.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

MK-2894 is a prostaglandin receptor 4 antagonist.MK-2894 has anti-inflammatory activity and may be used in the study of inflammation.

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

LX-7101 hydrochloride is a potent LIMK and ROCK2 inhibitor with antihypertensive activity, inhibits LIMK1/2, ROCK, PKA, and can be used to study glaucoma.

MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.