| Cat. No. |
Product Name |
CAS No. |
Information |
| H8934 |
Elinzanetant
|
929046-33-3 |
Elinzanetant (GSK1144814A) is a novel NK1 receptor and NK3 receptor antagonist for schizophrenia.with an estimated in vivo EC₅₀~0.9 ng/mL in the human brain. |
| H7416 |
MNKI-8e
|
1610886-04-8 |
MNKI-8e (MNK inhibitor 8e) is a potent, selective MNK inhibitor that inhibits Mnk2 with Ki of 0.37 uM, displays >34-fold and 4-fold over CDK2 (Ki>10 uM) and CDK9 (Ki=1.66 uM); potently inhibits leukemia cells with GI50 of 1.23-7.36 uM (MV4-11 GI50=1.32 uM and KG-1 GI50=1.23 uM); blocks phosphorylation of eIF4E, downregulates anti-apoptotic protein Mcl-1 and induces apoptosis in AML cells; suppresses the Ara-C-induced MAPK activity and enhances apoptosis in MV4-11 cells. |
| H7415 |
MNKI-85
|
1812885-57-6 |
MNKI-85 is a potent and selective Mnk2 inhibitor with Ki of 31 nM, displays no inhibitory activities against Mnk1, CDK2A, CDK9T, and CDK4D; effectively inhibits the growth of AML cells that possess an M5 subtype with FLT3-internal tandem duplication mutation, a powerful pharmacologic tool in studying the Mnk2/eIF4E-mediated tumorigenic mechanism. |
| H7414 |
MNKI-19
|
1211757-83-3 |
MNKI-19 is a potent and dual-specific Mnk inhibitor with Ki of 186 nM and 68 nM for Mnk1 and Mnk2, respectively; only displays moderate activity against Pim-1 (Ki=2.35 uM) in a panel of upstream activating kinases of Mnks, including B-Raf, MAPK1, MAPK2, Akt1, PI3K, p38α, and mTOR; inhibits the phosphorylation of eIF4E and 4E-BP1, arrests cancer cells in the G1 phase and induce apoptosis in FLT3-ITD expressed AML cells. |
| H7413 |
MNK-IN-54
|
1613168-64-1 |
MNK-IN-54 is a potent, orally bioavailable dual MNK1/2 and BCR-ABL1 inhibitor with IC50 of 20/10/200/10 nM for Abl T315I/ wt Abl/MNK1/MNK2, respectively; also inhibits RET, FLT3, VEGFR2 with IC50
|
| H7412 |
MNK inhibitor 9
|
1889336-59-7 |
MNK inhibitor 9 is a potent, selective MAPK-interacting kinase (MNK1 and MNK2) inhibitor with IC50 of 3 nM for both, with no activity aginst CDK1/2 (IC50>25 uM); displays excellent selectivity against a 53 kinase panel, with 4 kinases with IC50 <1 uM; inhibits eIF4E phosphorylation in KMS11-luc myeloma with IC50 of 0.6 nM, exhibits inhibition of cell proliferation in human multiple myeloma tumor cell line with EC50 of 1.7 uM; has good solubility and permeability, and is a suitable in vivo tool compound. |
| H7411 |
ETC-206
|
1464151-33-4 |
ETC-206 (ETC-1907206) is a novel potent, selective MNK1/2 inhibitor with IC50 of 64/86 nM, inhibits eIF4E phosphorylation inhibition in HeLa cell line with IC50 of 321 nM; displays excellent kinase selectivity, inhibits only 2 kinases by >65% at 1 uM against a panel of 104 kinases; demonstrates potent anti-proliferative activity against 25 hematological cancer cell lines with submicromolar IC50, especially against GK-5, DOHH2, AHH1 and P3HR-1 cell lines; prevents BC CML LSC self-renewal in vitro, significantly enhances the anti-tumor activity of dasatinib in BC CML mouse xenograft model.
|
| H7410 |
eFT508
|
1849590-01-7 |
eFT508 (Tomivosertib) is a potent, highly selective, reversible, ATP-competitive, and orally bioavailable MNK1 and MNK2 inhibitor with IC50 of 1-2 nM in enzyme assays; dose-dependently reduces eIF4E phosphorylation at Serine 209 in tumor cell lines with IC50 of 2-16 nM; shows anti-proliferative activity against multiple DLBCL cell lines, decreases the production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10; demonstrates significant anti-tumor activity in human lymphoma xenograft models which harbor activating MyD88 mutations. |
| H7409 |
CGP 57380
|
522629-08-9 |
A cell-permeable, specific MNK1 inhibitor with IC50 of 2.2 uM; has no inhibitory activity on p38, JNK1, ERK1/2, etc.; inhibits phosphorylation of eIF4E in cellular assays with IC50 of 3 uM. |
| H7408 |
Cercosporamide
|
131436-22-1 |
A broad-spectrum natural antifungal compound that acts as a selective and highly potent fungal Pkc1 kinase inhibitor; potent,y and ATP-competitively inhibits C. albicans Pkc (CaPkc1) kinase with IC50 of
|
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