| Cat. No. |
Product Name |
CAS No. |
Information |
| H9444 |
DTP3 trifluoroacetate
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway. |
| H9443 |
DTP3
|
1809784-29-9 |
DTP3 is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway. |
| H7384 |
Vacquinol-1
|
5428-80-8 |
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. |
| H7383 |
U0126-EtOH
|
1173097-76-1 |
U0126 (U0126-EtOH) is a potent, selective MEK (MAP2K) inhibitor with IC50 of 70 nM and 60 nM for MEK1 and MEK2, suppresses AP-1-mediated gene activation in transient transfection assays with IC50 of 0.96 uM; shows little to no effect on the kinase activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2, or Cdk4; inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs, but has no effect on IL-2-induced proliferation; reduces tumor size of tumor xenografts in nude mice. |
| H7382 |
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. |
| H7381 |
Trametinib
|
871700-17-3 |
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. |
| H7380 |
TAK-733
|
1035555-63-5 |
TAK-733 (TAK733,TAK 733) is a potent, selective, allosteric inhibitor of MEK with IC50 of 3.2 nM (MEK1); shows selectivity for MEK1 over a panel of 18 kinases, receptors, and ion channels at uM; inhibits ERK phosphorylation in vitro with EC50 of 1.9 nM, also inhibits proliferation of A375 and COLO 205 cells with IC50 of 3.1 nM and 2.1 nM, respectively; as well as 14 cutaneous melanoma cell lines (IC50s=<1-10 nM), espectially in those with B-RAFV600E mutations; demonstrates antitumor activity in multiple mouse xenograft models. |
| H7379 |
Selumetinib
|
606143-52-6 |
A highly potent and selective, ATP-uncompetitive inhibitor of MEK1/2 with IC50/Ki of 14.1 nM/22.6 nM for MEK1; shows no activity against other 40 serine/threonine and tyrosine kinases; inhibits cellular ERK1/2 phosphorylation (IC50<40 nM), suppresses growth inhibition of several cell lines containing B-Raf and Ras mutations (IC50=59-473 nM); causes growth of HT-29 xenograft tumors in nude mice. |
| H7378 |
RO4987655
|
874101-00-5 |
A potent and highly selective small-molecule MEK inhibitor with IC50 of 5.2 nM; exhibits anti-proliferation IC50s of 1-10 nM for COLO205 (CRC, Braf V600E), HT29 (CRC, Braf V600E), QG56 (NSCLC, HrasQ61L), MIA PaCa-2 (Panc, Kras G12C) cell lines. |
| H7377 |
RO-5126766
|
946128-88-7 |
Avutometinib is a potent, first-in-class dual Raf/MEK inhibitor with IC50 of 56 nM/160 nM for C-Raf/MEK1; shows weak or no inhibition on CYP2C9, CYP3A4 and hERG; inhibits ERK signaling output more effectively than a standard MEK inhibitor PD0325901 that induces MEK phosphorylation and has potent antitumor activity as well. |
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