Eleven-Nineteen-Leukemia Protein IN-3

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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

CAS No. : 2894121-83-4

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Description

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.

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	t_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (h•ng/mL)	AUC_0-∞ (h•ng/mL)	MRT_0-∞ (h)
p.o.	5.2	0.5	71.8	257	272	5.5
Administration	t_1/2 (h)	AUC_0-t (h•ng/mL)	AUC_0-∞ (h•ng/mL)	V_ss (L/kg)	CL (mL/min/kg)	MRT_0-∞ (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.

2894121-83-4

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

Handling Instructions (2659 KB)

References

[1]. Guo S, et al. Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC. Eur J Med Chem. 2023 Feb 15;248:115093. [Content Brief]