HMTase Inhibitor IX; MM-102

Code: 5006490001 D2-231

Biochem/physiol Actions

Reversible: yes

Primary TargetWDR5

Cell permeable: yes

General description

A cell-permeable peptidomimetic th...


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€305.40 EACH
€375.64 inc. VAT

Biochem/physiol Actions

Reversible: yes

Primary TargetWDR5

Cell permeable: yes

General description

A cell-permeable peptidomimetic that competes against MLL1 (Mixed Lineage Leukemia 1) minimum essential WIN (WDR5 INteracting) motif (-Ala3764-Arg-Ala3766-) for WDR5 (Trp-Asp Repeat Domain 5) binding (IC50/Ki = 2.5 nM/<1 nM and 540 nM/120 nM, respectively), effectively preventing MLL1 from complex assembling with WDR5, RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression (by 76% and 36%, respectively, after 96 h 50 µM MM-102 treatment) in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25 µM) via apoptosis induction (by >75% in 4 days in MV4:11 cultures; 50 µM MM-102), while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µM; >90 live cells after 4-day 50 µM MM-102 treatment).

A cell-permeable peptidomimetic that prevents MLL1 (Mixed Lineage Leukemia 1) from complex assembling with WDR5 (Trp-Asp Repeat Domain 5), RbBP5 (Retinoblastoma Binding Protein 5), and ASH2L (Absent Small or Homeotic-2-Like) for enhanced H3K4 methyltransferase activity (IC50 = 0.4 nM). Shown to reduce HoxA9 and Meis-1 mRNA expression in myeloblasts derived from MLL1-AF9-transduced murine bone marrow cells (50 µM for 96 h) and preferentially inhibit the growth of MLL1-AF4-harboring MV4;11 and MLL1-ENL-harboring KOPN8 leukemia cultures (GI50 in 7 days = 25 µM) via apoptosis induction, while exhibiting much reduced potency against BCR-ABL-dependent K562 cells (GI50 in 7 days = 84 µM).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Karatas, H., et al. 2013. J. Am. Chem. Soc.135, 669.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

Warning

Toxicity: Standard Handling (A)

assay≥95% (HPLC)
colorlight beige
formpowder
manufacturer/tradenameCalbiochem®
potency1 nM Ki
Quality Level100
solubilityDMSO: 100 mg/mL
storage conditiondesiccated (hygroscopic), protect from light, OK to freeze
storage temp.−20°C
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