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Eleven-Nineteen-Leukemia Protein IN-3

Catalog No. T72098 CAS 2894121-83-4

Eleven-Nineteen-Leukemia Protein IN-3, an orally active ENL YEATS domain inhibitor, exhibits potent activity with an IC50 of 15.4 nM. It downregulates MYC expression via ENL in cells and enhances ENL protein's thermal stability in vitro [1].

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Eleven-Nineteen-Leukemia Protein IN-3 Chemical Structure

Eleven-Nineteen-Leukemia Protein IN-3, CAS 2894121-83-4

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,820.00
50 mg	8-10 weeks	$ 2,380.00
100 mg	8-10 weeks	$ 3,100.00

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Description	Eleven-Nineteen-Leukemia Protein IN-3, an orally active ENL YEATS domain inhibitor, exhibits potent activity with an IC50 of 15.4 nM. It downregulates MYC expression via ENL in cells and enhances ENL protein's thermal stability in vitro [1].
Targets&IC50	Eleven-Nineteen-Leukemia YEATS domain:15.4 nM
In vitro	Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) exhibits significant inhibitory effects on the MV4-11 and MOLM-13 cell lines with IC50 values of 4.8 µM and 8.3 µM, respectively [1]. When applied at a concentration of 5 µM for 6 hours, it notably increases the thermal stability of the endogenous ENL protein, while it does not significantly affect the thermal stability of the GAS41 protein. Furthermore, Eleven-Nineteen-Leukemia Protein IN-3 effectively inhibits the growth of MOLM-13 cells [1]. At a concentration of 5 µM over 72 hours, it suppresses the expression of the crucial oncogene MYC by approximately 50%. In combination with JQ-1, Eleven-Nineteen-Leukemia Protein IN-3 further downregulates the expression of MYC in ENL target genes [1].
In vivo	Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) demonstrated oral bioavailability characteristics at a dose of 30 mg/kg when administered orally as a single dose [1]. When given intravenously at a dose of 5 mg/kg as a single injection, the compound exhibited higher systemic exposure in the body [1]. Pharmacokinetic (PK) studies in male BALB/c mice revealed the following parameters: for oral administration, the half-life (t 1/2) was 5.2 hours, time to peak concentration (T max) was 0.5 hours, maximum concentration (C max) was 71.8 ng/mL, area under the curve to the last measurable concentration (AUC 0-t) was 257 h•ng/mL, the extrapolated AUC (AUC 0-∞) was 272 h•ng/mL, and mean residence time (MRT 0-∞) was 5.5 hours. For intravenous administration, the t 1/2 was 4.0 hours, AUC 0-t was 8290 h•ng/mL, AUC 0-∞ was 8690 h•ng/mL, volume of distribution at steady state (V ss) was 0.8 L/kg, clearance (CL) was 9.6 mL/min/kg, MRT 0-∞ was 1.3 hours, and bioavailability (F %) was 0.5%.

Molecular Weight	465.55
Formula	C28H27N5O2
CAS No.	2894121-83-4

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Eleven-Nineteen-Leukemia Protein IN-3 2894121-83-4 Chromatin/Epigenetic Epigenetic Reader Domain inhibitor inhibit

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