2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. DOT1L705

DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia.
(Pink: DOT1L ligand (HY-135127); Blue: VHL E3 ligase ligand; Black: linker).

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

DOT1L705

DOT1L705 Chemical Structure

CAS No. : 3050756-34-5

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DOT1L705 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

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Description

DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia[1]. (Pink: DOT1L ligand (HY-135127); Blue: VHL E3 ligase ligand; Black: linker).

In Vitro

DOT1L705 (0.026-1 μM) inhibits H3K79 methylation, reduces viability of MLL-rearranged acute myeloid leukemia cell lines.
DOT1L808 (5-46.6 nM) inhibits H3K79 methylation, reduces viability of MLL-rearranged acute myeloid leukemia cell lines.

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

DOT1L705 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11
Concentration: 0-10 μM
Incubation Time: 6 h-96 h
Result: Induced dose-dependent degradation of DOT1L in MV-4-11 cells with a DC50 of 0.33 μM, achieving near-complete degradation within 4-6 hours (sustained for 96 hours).
Reduced H3K79me2 levels in MV-4-11 cells with an IC50 of 0.026 μM, 13-fold more potent than its effect on DOT1L protein levels.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: MLL-rearranged cell lines
Concentration: 0.01-100 μM
Incubation Time: 5 days
Result: Selectively inhibited viability of MLL-rearranged cell lines (MV-4-11 IC50 = 0.29 μM; EOL-1 IC50 = 0.39 μM; Pfeiffer IC50 = 0.80 μM) while showing minimal activity against non-MLL-rearranged lines (KG-1 IC50 > 50 μM).
In Vivo

DOT1L705 (1-10 mg/kg; i.p.; BID) demonstrates in vivo efficacy in an MV-4-11 xenograft model with favorable pharmacokinetic properties[1].

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

Animal Model: C57 BL/6 female mice ( 7−8 week old)[1]
Dosage: 1 mg/kg (pharmacokinetics); 10 mg/kg (in vivo efficacy)
Administration: in vitro; i.p. (single dose, pharmacokinetics); i.p. (BID, in vivo efficacy)
Result:
Reduced tumor volumes by >50% relative to vehicle control in an MV-4-11 subcutaneous xenograft model at 10 mg/kg BID i.p., with no significant body weight loss.
Showed reduced H3K79me2 levels in tumor lysates from the MV-4-11 subcutaneous xenograft model, confirming on-target activity.
Molecular Weight

1337.88

Formula

C61H72ClF3N12O13S2
CAS No.
SMILES

ClC1=C(N=CC=C1)[C@H](C2=C3OC(F)(OC3=CC=C2)F)NC4=C(C=C(C=C4)S(C)(=O)=O)NC5=NC(N6CCNCC6)=NC(OCCOCCOCCOCCOC7=CC(C8=C(N=CS8)C)=CC=C7CNC([C@@H]9C[C@H](CN9C([C@@H](NC(C%10(CC%10)F)=O)C(C)(C)C)=O)O)=O)=N5
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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DOT1L705 Related Classifications

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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:

DOT1L7053050756-34-5PROTACsHistone MethyltransferaseH3K79 methylationorthotopic modelsVHL E3 ubiquitin ligaseMLL-rearranged acute myeloid leukemia cell linesDOT1Lproteasomal degradationMV-4-11 xenograft modelMLL-rearranged leukemia cellsmenin inhibitor-resistant leukemia cellsInhibitorinhibitorinhibit

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