trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation[1].
Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK inhibitor with an IC50 of 4.2 nM for MEK1.
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions[1].
SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
GW284543 (UNC10225170) is a selective MEK5 inhibitor[1].
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines[1].
GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis[1].
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. Nedometinib has antineoplastic effect and can be used for research in dermatosis, cutaneous fibroneuroma, neurofibromatosis[1].
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy[1][2].
Ro 5126766 is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway[1].
EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
Trametinib is a potent MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Due to the poor solubility of Trametinib, Trametinib DMSO solvate (Cat. No.: HY-10999A) is recommeded.
(R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo[1].
(E/Z)-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; (E/Z)-Zeatin also inhibits UV-induced MEK/ERK activation.
Lidocaine, an amide local anesthetic, has anti-inflammatory properties in vitro and in vivo, possibly due to an attenuation of pro-inflammatory cytokines, intracellular adhesion molecule-1 (ICAM-1), and reduction of neutrophils influx.Target: Lidocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name xylocaine by Swedish chemist Nils Lofgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself.Lidocaine is approximately 95% metabolized (dealkylated) in the liver by CYP3A4 to the pharmacologically-active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half life than lidocaine but also is a less potent sodium channel blocker. The elimination half-life of lidocaine is approximately 90–120 minutes in most patients. This may be prolonged in patients with hepatic impairment (average 343 minutes) or congestive heart failure (average 136 minutes).
GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein[1].
U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM[1].
PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].
PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects[1].
Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor with an IC50 of 12 nM.