MNK/PIM-IN-2
MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC50 of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3081482-46-1
- Formule: C26H28FN7O2
- Masse moléculaire:489.54
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform Caspase
More
Activité biologique
Description
In Vitro
MNK/PIM-IN-2 (compound 2j) inhibits the proliferation of human leukemia cell lines MOLM-13, THP-1, U937 and K562 after 72 h[1].
MNK/PIM-IN-2 (1-2 μM; 12-24 h) induces G0/G1 phase arrest in human leukemia cell lines MOLM-13 and K562[1].
MNK/PIM-IN-2 (1-2 μM; 12-24 h) induces apoptosis in the human leukemia cell line MOLM-13, but exerts no significant apoptotic effect on the human leukemia cell line K562[1].
MNK/PIM-IN-2 (2 μM; 12-24 h) inhibits the Pim/Mnk signaling pathway in human leukemia cells MOLM-13 and K562, reduces the levels of p-eIF4E and p-4EBP1, downregulates the expression of Mcl-1 and c-Myc, and induces PARP cleavage in MOLM-13 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human leukemia cell lines (MOLM-13, THP-1, U937, K562)
-
Concentration:/
-
Incubation Time:72 h
-
Result:Exhibited potent antiproliferative activity against MOLM-13 cells with a GI50 value of 0.19 μM.
Exhibited potent antiproliferative activity against THP-1 cells with a GI50 value of 1.04 μM.
Exhibited potent antiproliferative activity against U937 cells with a GI50 value of 0.59 μM.
Exhibited potent antiproliferative activity against K562 cells with a GI50 value of 0.70 μM.
-
Cell Line:Human leukemia cell lines (MOLM-13, K562)
-
Concentration:1, 2 μM
-
Incubation Time:12 h (MOLM-13); 24 h (K562)
-
Result:Induced G0/G1 phase arrest in MOLM-13 cells at 1 μM for 12 h, with 65.32% of cells in G0/G1.
Caused substantial accumulation in the sub-G1 phase in MOLM-13 cells at 2 μM for 12 h, with 40.44% of cells in sub-G1.
Induced G0/G1 phase arrest in K562 cells at 1 μM for 24 h.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Balb-c/nu (female) with subcutaneous MOLM‑13 cell inoculation to establish leukemia xenografts[1]
-
Dosage:10 mg/kg; 20 mg/kg
-
Administration:daily; 2 weeks
-
Result:Suppressed tumor growth with an inhibition rate of 57.1%.
Suppressed tumor growth with an inhibition rate of 72.6%.
Reduced Ki67 expression in tumor tissues.
Upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant changes in mouse body weight during administration.
Showed no abnormal changes in major organs via pathological analysis.
Chemical Information
-
CAS No. 3081482-46-1
-
Masse moléculaire 489.54
-
Formule C26H28FN7O2
-
SMILES
FC1=CC(OC2CCOCC2)=C(NC3=C4C(C=CC(C5=CN(N=C5)C6CCNCC6)=N4)=NC=N3)C=C1
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MNK/PIM-IN-2 Related Classifications
HY-182957 Related Classifications
Powered by Bioz