• 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
S1008 Selumetinib (AZD6244) <1 mg/mL 91 mg/mL <1 mg/mL
S1036 PD0325901 <1 mg/mL 96 mg/mL 40 mg/mL
S1020 PD184352 (CI-1040) <1 mg/mL 96 mg/mL 14 mg/mL
S1177 PD98059 <1 mg/mL 14 mg/mL <1 mg/mL
S1531 BIX 02189 <1 mg/mL 60 mg/mL 80 mg/mL
S1475 Pimasertib (AS-703026) <1 mg/mL 86 mg/mL <1 mg/mL
S1530 BIX 02188 <1 mg/mL 43 mg/mL 3 mg/mL
S2617 TAK-733 <1 mg/mL 101 mg/mL <1 mg/mL
S2134 AZD8330 <1 mg/mL 92 mg/mL 92 mg/mL
S7007 Binimetinib (MEK162, ARRY-162, ARRY-438162) <1 mg/mL 88 mg/mL <1 mg/mL
S1568 PD318088 <1 mg/mL 112 mg/mL 14 mg/mL
S2310 Honokiol <1 mg/mL 53 mg/mL <1 mg/mL
S1089 Refametinib (RDEA119, Bay 86-9766) <1 mg/mL 100 mg/mL 100 mg/mL
S2326 Myricetin <1 mg/mL 63 mg/mL 9 mg/mL
S7843 BI-847325 <1 mg/mL 19 mg/mL 1 mg/mL
S8041 Cobimetinib (GDC-0973, RG7420) <1 mg/mL 100 mg/mL 47 mg/mL
S7553 GDC-0623 <1 mg/mL 91 mg/mL 5 mg/mL
S8355 APS-2-79 HCl <1 mg/mL 97 mg/mL 32 mg/mL


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

Selumetinib (AZD6244)

Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.



PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.


PD184352 (CI-1040)

PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.



PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.


BIX 02189

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.


Pimasertib (AS-703026)

Pimasertib (AS-703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines. Phase 2.


BIX 02188

BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.



TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.



AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.


Binimetinib (MEK162, ARRY-162, ARRY-438162)

Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.



PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.



Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.


Refametinib (RDEA119, Bay 86-9766)

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.



Myricetin, a natural flavonoid with antioxidant and anti tumor properties, is a novel inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells. It also inhibits PI3Kγ with Kd of 0.17 μM.



BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.


Cobimetinib (GDC-0973, RG7420)

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.



GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.


APS-2-79 HCl

APS-2-79 is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK.

Tags: MEK inhibition | MEK pathway | MEK activation | MEK inhibitor cancer | MEK phosphorylation | MEK activity | MEK inhibitor clinical trial | MEK inhibitor side effects | MEK inhibitor drugs | MEK inhibitor review