2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. DOT1L808

DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model.
(Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).

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

DOT1L808

DOT1L808 Chemical Structure

Size Price Stock Quantity
1 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 7 - 9 weeks
5 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 7 - 9 weeks
10 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 7 - 9 weeks
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Customer Review

Based on 1 publication(s) in Google Scholar

DOT1L808 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

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Description

DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model[1]. (Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).

IC50 & Target[1]

VHL

 

DOT1L

5 nM (DC50)

In Vivo

DOT1L808 (25 mg/kg; i.p.; twice daily; 5 days per week for 2 weeks) significantly inhibits tumor growth in the MV-4−11-Luc acute myeloid leukemia model of NSG mice[1].

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

Animal Model: NSG mice (female, 6-8 weeks old, tail vein injection of 1.5 × 106 MV-4−11-Luc cells)[1]
Dosage: 25 mg/kg
Administration: i.p.; twice daily; 2 weeks (5 days per week)
Result: Markedly reduced bioluminescent signal (total photon flux per second) relative to vehicle-treated mice, indicating significant inhibition of disseminated leukemia growth.
Showed no significant body weight changes compared to vehicle controls.
Molecular Weight

1301.89

Formula

C61H72ClF3N14O9S2
SMILES

CC1=C(SC=N1)C2=CC=C(C(OCCN3CCN(CC3)CCN4CCN(CC4)C5=NC=NC(NC6=C(C=CC(S(C)(=O)=O)=C6)N[C@H](C7=C(C=CC=N7)Cl)C8=C9OC(F)(OC9=CC=C8)F)=N5)=C2)CNC([C@@H]%10C[C@H](CN%10C([C@H](C(C)(C)C)NC(C%11(CC%11)F)=O)=O)O)=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
References
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DOT1L808 Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DOT1L808PROTACsHistone MethyltransferaseH3K79 methylationH3K79me2NSG miceMLL-rearranged leukemiaVHL E3 ubiquitin ligaseproteasomal degradationMV-4?11-Luc acute myeloid leukemiaMV-4?11 acute myeloid leukemiaDOT1Lleukemia cellsInhibitorinhibitorinhibit

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HY-181789
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