| Cat. No. |
Product Name |
Information |
| PC-21799 |
HRX-0233
MAP2K4 inhibitor
|
HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers. |
| PC-21237 |
NFX-179
MEK inhibitor
|
NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1). |
| PC-20654 |
DK2403
MAP2K7 inhibitor
|
DK2403 (DK-2403) is a highly potent, selective and covalent MAP2K7 (MEK7) inhibitor with IC50 of 10 nM, covalently engages the unique Cys218 residue within the active site. |
| PC-20026 |
HRX215
MKK4 inhibitor
|
Darizmetinib (HRX215, HRX0215) is a first-in-class, potent, selective inhibitor of MKK4 (mitogen-activated protein kinase kinase 4, MEK4, MAP2K4) with IC50 of 20 nM, >100-fold selectivity against JNK1, BRAF, and MKK7. |
| PC-49771 |
Binimetinib
MEK inhibitor
|
Binimetinib (ARRY-162, ARRY-438162, MEK162) is a potent, selective and non-competitive inhibitor of MEK1/2 with IC50 of 12 nM in cell-free assays. |
| PC-49634 |
DS03090629
MEK inhibitor
|
DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM). |
| PC-38901 |
KZ-001
MEK inhibitor
|
KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244. |
| PC-38495 |
(R)-STU104
TAK1-MKK3 PPI inhibitor
|
(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3. |
| PC-38429 |
Zapnometinib
MEK inhibitor
|
Zapnometinib (ATR-002, PD0184264) is the active metabolite of CI-1040, a novel MEK inhibitor (IC50=30.96 nM, cell free assay) with broad antiviral activity against different influenza virus strains, as well as SARS-CoV-2. |
| PC-38424 |
Tunlametinib
MEK inhibitor
|
Tunlametinib (HL-085) is a highly selective and potent MEK inhibitor with IC50 of 1.9 nM (MEK1), exhibits potent activity against RAS/RAF mutant cancer cells. |
| PC-38417 |
BT2
Angiogenesis inhibitor
|
BT2 is a thermostable small-molecule inhibitor of vascular permeability and angiogenesis, interacts with MEK1 and inhibits ERK phosphorylation, FosB/ΔFosB, and VCAM-1 expression. |
| PC-73276 |
INR119
MEK1/2 inhibitor
|
INR119 is a small molecule allosteric MAPKK (MAP2K, MEK1/2) inhibitor, binds fission yeast homologue Wis1 near C458 and protects Wis1 from inactivation by low levels of H2O2 in vitro. |
