About 31 results found for searched term "MK2-IN-5" (0.089 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M49716 | MK2-IN-5 | ERK |
| MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). | ||
| M1822 | PD98059 | MEK |
| PD 98059; PD‐98059 | ||
| PD98059 is a potent and selective inhibitor of mitogen-activated protein kinase kinase (MKK / MEK) with IC50 value of 2-7 μM. The expression of KAT2B protein in cells is significantly decreased after PD98059 inhibits ERK signaling pathway. | ||
| M1837 | MK-2206 2HCl | Akt |
| MK-2206 dihydrochloride | ||
| MK-2206 is a novel allosteric inhibitor of Akt with IC50 values of 8 nM, 12 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. | ||
| M1985 | Odanacatib | Cathepsin |
| MK-0822 | ||
| Odanacatib (MK-0822) is a potent and reversible covalent inhibitor of CathepsinK (CatK) with an IC50 of 0.2 nM/1 nM for human/rabbit cathepsin B, L, and S and is highly selective. | ||
| M2120 | MK-0752 | Gamma-secretase/Beta-secretase |
| MK-0752 is a potent, oral inhibitor of γ-secretase with IC50 of 5 nM in human SH-SY5Y cells. | ||
| M2203 | Elbasvir | HCV Protease |
| MK-8742 | ||
| Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) replication complex inhibitor, with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively. | ||
| M2215 | Niraparib (MK-4827) | PARP |
| MK-4827 | ||
| MK-4827 (Niraparib) is a selective PARP1/2 inhibitor with an IC50 value of 3.8 nM/2.1 nM that increases the formation of PARP-DNA complexes through inhibition of PARPase activity, leading to DNA damage, apoptosis, PARP-1-dependent cell death (parthanatos) and cell death. Strong effector activity when acting on cancer cells harboring mutant BRCA-1 and BRCA-2. It is more than 330-fold more selective than PARP3, V-PARP and Tank1. | ||
| M2256 | Ivermectin (MK-933) | Autophagy |
| Stromectol; MK-933; CD-5024; K-237 | ||
| Ivermectin (MK-933) is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor and the purinergic P2X4 receptor. Importin α5 inhibitor ivermectin effectively abrogates STAT1-importin α5 interactions. | ||
| M2595 | Raltegravir | Integrase |
| MK-0518 | ||
| Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. | ||
| M3195 | MK-2048 | Integrase |
| MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. | ||
| M3278 | MK-5172 (Grazoprevir) | HCV Protease |
| Grazoprevir; MK5172 | ||
| MK-5172 is a novel NS3/4, a protease inhibitor for chronic HCV infection (Enzyme Ki for genotype1b, 2a, 2b and 3a at ＜0.02, 0.15, 0.02 and 0.7 nM, respectively). | ||
| M3515 | MK-2461 | c-Met |
| MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. | ||
| M3518 | MK-8245 | Stearoyl-CoA Desaturase |
| MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. | ||
| M4936 | Omarigliptin | Dipeptidyl Peptidase |
| MK-3102 | ||
| Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 _mu_M). | ||
| M4986 | LMK-235 | HDAC |
| LMK235 is a HDAC inhibitor, previously shown to be a novel and specific inhibitor of human HDAC4 and 5, with IC50 values of 0.49 μM (A2780) and 0.32 μM (A2780 CisR). | ||
| M8926 | Niraparib (MK-4827) tosylate | PARP |
| MK-4827 tosylate | ||
| Niraparib (MK-4827) tosylate is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively. | ||
| M9499 | TH-257 | LIM Kinase |
| TH257 | ||
| TH-257 is a potent and selective allosteric LIMK 1/2 inhibitor with IC50 values of 84 nM and 39 nM, respectively. | ||
| M9803 | MK-8353 | ERK |
| SCH900353 | ||
| MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK1/2 inhibitor, with IC50 values of 23.0 nM and 8.8 nM, respectively. | ||
| M10858 | MK-2894 | Prostaglandin Receptor |
| MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis. | ||
| M10957 | MK-0429 | Integrin |
| L-000845704 | ||
| MK-0429 (L-000845704) is an oral, highly effective, selective, non-peptide integrin ubiquitous antagonist for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1 IC5 0 The values are 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM, and 12.2 nM, respectively. | ||
| M13711 | Niraparib hydrochloride | PARP |
| MK-4827 hydrochloride | ||
| Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. | ||
| M13729 | LX7101 | ROCK |
| LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM. | ||
| M13986 | MK-6892 | Others |
| MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively. | ||
| M14044 | MK-2894 sodium salt | Prostaglandin Receptor |
| MK-2894 sodium salt is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). | ||
| M14165 | MK2-IN-1 hydrochloride | MAPKAPK2/MAP3K/MAP4K |
| MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. | ||
| M14536 | MK-8245 Trifluoroacetate | Others |
| MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. | ||
| M20793 | Amitriptyline | Serotonin Transporter |
| MK-230; N-750; Ro41575 | ||
| Amitriptyline (MK-230, N-750, Ro41575) is an inhibitor of the serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki values of 3.45 nM and 13.3 nM, respectively, and also inhibits the histamine receptor H1, the histamine receptor H4, 5-HT2, and the Sigma 1 receptor with Ki values of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. It can also inhibit histamine receptor H1, histamine receptor H4, 5-HT2 and Sigma 1 receptor with Ki values of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively, and can be used in studies of depression and neuropathic pain. | ||
| M21038 | MK2 Inhibitor III | p38 MAPK |
| MK2-IN-3 | ||
| MK2 Inhibitor III (MK2-IN-3) is an ATP-competitive MK2 (MAPKAP-K2) inhibitor with an IC50 value of 8.5 nM. | ||
| M27685 | Niraparib (R-enantiomer) | PARP |
| MK 4827 (R-enantiomer) | ||
| Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM. | ||
| M27831 | MK-0941 | Glucokinase (GK) |
| MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes. | ||
| M27943 | Grazoprevir potassium salt | HCV Protease |
| MK-5172 potassium salt | ||
| Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir potassium salt inhibits SARS-CoV-2 3CLpro activity. | ||
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