1. Epigenetics
  2. Histone Methyltransferase
  3. Dot1L-IN-4

Dot1L-IN-4 

Cat. No.: HY-135127
Handling Instructions

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.

For research use only. We do not sell to patients.

Dot1L-IN-4 Chemical Structure

Dot1L-IN-4 Chemical Structure

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Description

Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM[1].

IC50 & Target

DOT1L

0.11 nM (IC50)

In Vitro

Dot1L-IN-4 (Compound 10) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=1.7 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=33 nM). Dot1L-IN-4 also inhibits mixed lineage leukemia (MLL) with an IC50 of 99 µM[1].

In Vivo

Dot1L-IN-4 (Compound 10; 300 mg/kg; p.o.; qd) is not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA are reduced only by less than half as compared to control animals[1].

Animal Model: Male mice (C57BL/6) bearing subcutaneous MV4-11 tumor xenografts[1]
Dosage: 300 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Was not tolerated at such a high dose by tumor xenograft bearing mice, and at a 6-fold reduced dose, the tumor growth as well as the HOXA9 reporter gene mRNA were reduced only by less than half as compared to control animals.
Molecular Weight

661.08

Formula

C₂₈H₂₇ClF₂N₈O₅S

SMILES

O=S(C1=CC=C(N[[email protected]](C2=NC=CC=C2Cl)C3=C4OC(F)(F)OC4=CC=C3)C(NC5=NC(OC)=NC(N6CCNCC6)=N5)=C1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Dot1L-IN-4Histone MethyltransferaseDOT1LH3K79lysinehistonemethyltransferaseInhibitorinhibitorinhibit

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Dot1L-IN-4
Cat. No.:
HY-135127
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