Eleven-Nineteen-Leukemia Protein IN-3 NEW
| Price | $1820 | $2380 | $3100 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Eleven-Nineteen-Leukemia Protein IN-3 | CAS No.: 2894121-83-4 |
| Supply Ability: 10g | Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Eleven-Nineteen-Leukemia Protein IN-3 |
| 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]. |
| In vitro | Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) exhibits significant inhibitory effects on MV4-11 and MOLM-13 cell lines with IC50 values of 4.8 μM and 8.3 μM, respectively [1]. At 5 μM for 6 hours, it increases the thermal stability of the endogenous ENL protein without impacting GAS41 protein stability. Additionally, it inhibits MOLM-13 cell growth [1], suppressing MYC oncogene expression by approximately 50% at 5 μM over 72 hours. When combined with JQ-1, it further downregulates MYC expression in ENL target genes [1]. |
| In vivo | Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) demonstrated oral bioavailability at a dose of 30 mg/kg when administered orally as a single dose [1]. When given intravenously at 5 mg/kg as a single injection, the compound showed higher systemic exposure [1]. Pharmacokinetic (PK) studies in male BALB/c mice revealed that for oral administration, the half-life (t 1/2) was 5.2 hours, with a time to peak concentration (T max) of 0.5 hours, a maximum concentration (C max) of 71.8 ng/mL, an area under the curve to the last measurable concentration (AUC 0-t) of 257 h?ng/mL, an extrapolated AUC (AUC 0-∞) of 272 h?ng/mL, and a mean residence time (MRT 0-∞) of 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%. |
| Storage | Shipping with blue ice. |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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