ERK

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S7752New

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

S7752New

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.