1. Epigenetics
  2. Histone Methyltransferase
  3. Dot1L-IN-5

Dot1L-IN-5 

Cat. No.: HY-135128
Handling Instructions

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.

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

Dot1L-IN-5 Chemical Structure

Dot1L-IN-5 Chemical Structure

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Description

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM[1].

IC50 & Target

DOT1L

0.17 nM (IC50)

In Vitro

Dot1L-IN-5 (Compound 11) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED50 H3K79me2 Elisa=2.9 nM) and HOXA9 gene expression in Molm-13 cells (ED50 HOXA9 RGA=30 nM)[1].

In Vivo

Dot1L-IN-5 (Compound 11; subcutaneous injection; at 75 mg/kg once daily for 20 days) does not lead to tumor growth inhibition in NOD-SCID mice. Dot1L-IN-5 (subcutaneous injection; at 75 mg/kg twice daily for 20 days) leads 73% growth inhibition[1].
While both treatment regimens result in very strong inhibition of global H3K79 dimethylation level in tumor, the efficacious regimen is superior in reducing the mRNA expression of the target genes HOXA9 and MEIS1[1].

Animal Model: NOD-SCID mice bearing subcutaneous MV4-11 tumor xenografts[1]
Dosage: 75 mg/kg
Administration: Subcutaneous injection; at 75 mg/kg once or twice daily for 20 days
Result: Once daily administration did not lead to tumor growth inhibition, 73% growth inhibition was measured in the twice daily treated group.
Molecular Weight

592.96

Formula

C₂₃H₁₉ClF₂N₈O₅S

SMILES

O=S(C1=CC=C(N[[email protected]](C2=NC=CC=C2Cl)C3=C4OC(F)(F)OC4=CC=C3)C(NC5=NC(N)=NC(OC)=N5)=C1)(N)=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-5Histone MethyltransferaseDOT1LH3K79lysinehistonemethyltransferaseInhibitorinhibitorinhibit

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Dot1L-IN-5
Cat. No.:
HY-135128
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