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Cat. No.: HY-135129

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Dot1L-IN-6

Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.19 nM.

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

CAS No.: 2565705-01-1
Formula: C₂₅H₂₁ClF₂N₆O₆S
Molecular Weight:606.99

Storage:

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

Data Sheet (272 KB)

Dot1L-IN-6 Chemical Structure

CAS No.: 2565705-01-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC_{50 SPA DOT1L} of 0.19 nM^[1].

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	ED₅₀	12 nM Compound: 9	Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79 dimethylation measured after 72 hrs by ELISA Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79 dimethylation measured after 72 hrs by ELISA	[PMID: 31857842]

In Vitro

Dot1L-IN-6 (Compound 9) is tested in cellular assays to assess the ability to inhibit the dimethylation of H3K79 in HeLa cells (ED_{50 H3K79me2 Elisa}=12 nM) and HOXA9 gene expression in Molm-13 cells (ED_{50 HOXA9 RGA}=170 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dot1L-IN-6 (Compound 9) shows an excellent blood exposure after a single dose (100 mg/kg)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2565705-01-1
Molecular Weight 606.99
Formula C₂₅H₂₁ClF₂N₆O₆S
SMILES

O=S(C1=CC=C(N[C@H](C2=NC=CC=C2Cl)C3=C4OC(F)(F)OC4=CC=C3)C(NC5=NC(OC)=NC(OC)=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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Frédéric Stauffer, et al. New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse. ACS Med. Chem. Lett. 2019, 10, 12, 1655-1660.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Dot1L-IN-6

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Dot1L-IN-6 Related Classifications

HY-135129 Related Classifications