2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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.

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Eleven-Nineteen-Leukemia Protein IN-3 Chemical Structure

Eleven-Nineteen-Leukemia Protein IN-3 Chemical Structure

CAS No. : 2894121-83-4

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Eleven-Nineteen-Leukemia Protein IN-3 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Eleven-Nineteen-Leukemia YEATS domain

15.4 nM (IC50)

In Vitro

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.

Eleven-Nineteen-Leukemia Protein IN-3 Related Antibodies

RT-PCR[1]

Cell Line: MOLM-13 cells.
Concentration: 5 µM.
Incubation Time: 72 h.
Result: Showed inhibitory for MYC.
In Vivo

Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) (30 mg/kg; p.o.; single dose) shows oral exposure characteristics[1].
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.

Animal Model: Male BALB/c mice[1].
Dosage: 30 mg/kg.
Administration: Oral gavage; single dose.
Result: Showed an oral activity.
Animal Model: Male BALB/c mice[1].
Dosage: 5 mg/kg.
Administration: Intravenous injection; single dose.
Result: Exhibited efficacy.
Molecular Weight

465.55

Formula

C28H27N5O2
CAS No.
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
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Eleven-Nineteen-Leukemia Protein IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eleven-Nineteen-Leukemia Protein IN-32894121-83-4Epigenetic Reader DomainMV4-11MOLM-13Male BALB/c miceInhibitorinhibitorinhibit

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