| Cat. No. |
Product Name |
CAS No. |
Information |
| GY04370 |
Vacquinol-1
|
5428-80-8(freebase） |
Vacquinol-1 (NSC 13316) is a MKK4 (MAP2K4, MEK4) activator that induces vacuolization, induces ATP depletion in glioblastoma cells (IC50 = 3.14 uM) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells; induces rapid and specific cell death of glioma cells via membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture; shows good brain penetrance and excellent pharmacokinetics; orally bioactive. |
| GY02971 |
APS-2-79
|
2002381-25-9 |
A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization, and the conformational changes required for phosphorylation and activation of KSR-bound MEK (KSR2 IC50=120 nM); binds to the KSR2-MEK1 complex and impedes the assembly of RAF–KSR–MEK complexes, suppresses KSR-stimulated MEK and ERK phosphorylation and suppresses oncogenic Ras mutations; enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations. |
| GY10219 |
MKK7-COV-3
|
|
MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases, with very few kinases inhibited by more than 75% at 1 uM: Aurora kinase B, LRRK2, and MKK4, as well as FLT3; inhibits 60% of the CD86+ response in primary mouse B cells in response to LPS stimulation (10 μM, 2 hr pre-incubation). |
| GY10220 |
MKK7-COV-13
|
|
MKK7-COV-13 (MKK7 Covalen inhibitor 13) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 10 nM, displays >1,000-fold selectivity over MKK4 (IC50>10 uM); shows EC50 of 0.3-1.0 uM for reduction of p-JNK in HEK293 cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation. |
| GY10221 |
MKK7-COV-9
|
|
MKK7-COV-9 (MKK7 Covalen inhibitor 9) is a potent, selective, covalent MKK7 inhibitor, displays >1,000-fold selectivity over MKK4; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation (EC50=4.9 uM); has half-lives >40 min in dog and rat, and significantly improved stability in human and monkey liver microsomes; MKK7-COV-9 is not cytotoxic to a panel of human cell lines. |
| GY10480 |
MMK7 inhibitor 4a
|
|
MMK7 inhibitor 4a is a potent, sepecific, covalent inhibitor of MMK7, displays >800-fold selectivity over EGFR-WT and EGFR-L858R/T790M; MMK7 inhibitor 4a formed a covalent bond to Cys218 at the end of the hinge region of MMK7; displayed an excellent selectivity profile at 1 uM against a panel of 320 kinases; potently inhibits cellular JNK at 1 uM and completely inhibited its downstream effector c-Jun with no effect on the JNK-pathway; MMK7 inhibitor 4a is a valuable
probe for further investigation to elucidate the function of MKK7 in cellular studies and in vivo. |
| GY02331 |
BIX02189
|
1265916-41-3 |
BIX02189 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity (IC50=59 nM), does not inhibits closely related kinases MEK1, MEK2, ERK2, and JNK2; ; blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells, also inhibits transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade; blocks ERK5 signaling and suppresses NGF-induced neurite outgrowth in PC12 cells. |
| GY02209 |
Trametinib DMSO solvate
|
1187431-43-1 |
A potent and highly specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM; exhibits no inhibition on the kinase activities of c-Raf, B-Raf, ERK1/2. |
| GY01860 |
APS-2-79 hydrochloride
|
2002381-31-7 |
A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization, and the conformational changes required for phosphorylation and activation of KSR-bound MEK (KSR2 IC50=120 nM); binds to the KSR2-MEK1 complex and impedes the assembly of RAF–KSR–MEK complexes, suppresses KSR-stimulated MEK and ERK phosphorylation and suppresses oncogenic Ras mutations; enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations. |
| GY03727 |
Cobimetinib racemate
|
934662-91-6 |
Cobimetinib racemate is the racemate form of Cobimetinib (GDC-0973, XL518), which is a potent, highly selective inhibitor of MEK1/2. |
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