Eleven-Nineteen-Leukemia Protein IN-3
Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro.
For research use only. We do not sell to patients.
- CAS No.: 2894121-83-4
- Formula: C28H27N5O2
- Molecular Weight:465.55
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Eleven-Nineteen-Leukemia YEATS domain 15.4 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
8.3 μM
Compound: 28
|
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by Cell Titer-Glo luminescent assay
|
[PMID: 36645983] |
| MV4-11 | IC50 |
4.8 μM
Compound: 28
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by Cell Titer-Glo luminescent assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by Cell Titer-Glo luminescent assay
|
[PMID: 36645983] |
Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) has significant inhibitory effect on MV4-11 and MOLM-13 cell lines with IC50 values of 4.8 μM and 8.3 μM, respectively[1].
Eleven-Nineteen-Leukemia Protein IN-3 (5 µM; 6 h) significantly improves the thermal stability of endogenous ENL protein, but has insignificant effect on the thermal stability of GAS41 protein. Eleven-Nineteen-Leukemia Protein IN-3 can effectively inhibits the growth of MOLM-13 cells[1].
Eleven-Nineteen-Leukemia Protein IN-3 (5 µM; 72 h) inhibits the key oncogene MYC (about 50 %). Eleven-Nineteen-Leukemia Protein IN-3 can further down-regulates the expression of MYC in the ENL target gene when works with JQ-1 (HY-13030)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MOLM-13 cells.
-
Concentration:5 µM.
-
Incubation Time:72 h.
-
Result:Showed inhibitory for MYC.
Eleven-Nineteen-Leukemia Protein IN-3 (5 mg/kg; i.v.; single dose) highly exposes in vivo[1].
Pharmacokinetic (PK) study in Male BALB/c mice[1]
| Administration | t1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (h•ng/mL) | AUC0-∞ (h•ng/mL) | MRT0-∞ (h) | |
| p.o. | 5.2 | 0.5 | 71.8 | 257 | 272 | 5.5 | |
| Administration | t1/2 (h) | AUC0-t (h•ng/mL) | AUC0-∞ (h•ng/mL) | Vss (L/kg) | CL (mL/min/kg) | MRT0-∞ (h) | F (%) |
| i.v. | 4.0 | 8290 | 8690 | 0.8 | 9.6 | 1.3 | 0.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2894121-83-4
-
Molecular Weight 465.55
-
Formula C28H27N5O2
-
SMILES
C[C@H]1CCCN1CC2=NC3=CC(NC(C4=CC=C5C(C6=CC=CC=C6C(N5C)=O)=C4)=O)=CC=C3N2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Eleven-Nineteen-Leukemia Protein IN-3 Related Classifications
HY-152471 Related Classifications
Powered by Bioz