ERK

シグナル伝達経路

研究分野

  • 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S7101 SCH772984 <1 mg/mL 14 mg/mL <1 mg/mL
S7921 DEL-22379 <1 mg/mL 89 mg/mL <1 mg/mL
S8701 MK-8353 (SCH900353) <1 mg/mL 50 mg/mL <1 mg/mL
S8708 AZD0364 <1 mg/mL 99 mg/mL 99 mg/mL
S7709 VX-11e <1 mg/mL 100 mg/mL 16 mg/mL
S8801 CC-90003 <1 mg/mL 92 mg/mL <1 mg/mL
S9306 Corynoxeine -1 mg/mL 76 mg/mL -1 mg/mL
s9102 Magnolin -1 mg/mL 83 mg/mL -1 mg/mL
S7334 ERK5-IN-1 <1 mg/mL 100 mg/mL 100 mg/mL
S7525 XMD8-92 <1 mg/mL 73 mg/mL <1 mg/mL
S8534 LY3214996 <1 mg/mL 27 mg/mL 16 mg/mL
S7752 SC1 <1 mg/mL 100 mg/mL <1 mg/mL
S7854 Ulixertinib (BVD-523, VRT752271) <1 mg/mL 86 mg/mL 15 mg/mL
S7524 FR 180204 <1 mg/mL 65 mg/mL 2 mg/mL
S7554 GDC-0994 <1 mg/mL 87 mg/mL 87 mg/mL

亜型選択性的な製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7101

SCH772984

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.

S7921

DEL-22379

DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.

S8701

MK-8353 (SCH900353)

MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).

S8708

AZD0364

AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.

S7709

VX-11e

VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.

S8801

CC-90003

CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.

S9306

Corynoxeine

Corynoxeine, which could be isolated from Uncaria rhynchophylla, is a useful and prospective compound in the prevention and treatment for vascular diseases. It is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation.

s9102

Magnolin

Magnolin is a natural compound abundantly found in Magnolia flos targeting ERK1 (IC50=87 nM) and ERK2 (IC50=16.5 nM) and inhibits cell transformation induced by tumor promoters such as epidermal growth factor (EGF).

S7334

ERK5-IN-1

ERK5-IN-1 is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.

S7525

XMD8-92

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.

S8534

LY3214996

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

S7752

SC1

Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. Maintains embryonic stem cell (ESC) self-renewal.

S7854

Ulixertinib (BVD-523, VRT752271)

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

S7524

FR 180204

FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.

S7554

GDC-0994

GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.