An inhibitor of MLLT1 and MLLT3 YEATS domains
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SGC-iMLLT

Item No. 28113

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-N-[2-[[(2S)-2-methyl-1-pyrrolidinyl]methyl]-1H-benzimidazol-6-yl]-1H-indazole-5-carboxamide
CAS Number
2255338-25-9
Molecular Formula
C22H24N6O
Formula Weight
388.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
234, 295 nm
SMILES
CN(N=C1)C2=C1C=C(C(NC3=CC(N=C(CN4CCC[C@@H]4C)N5)=C5C=C3)=O)C=C2
InChi Code
InChI=1S/C22H24N6O/c1-14-4-3-9-28(14)13-21-25-18-7-6-17(11-19(18)26-21)24-22(29)15-5-8-20-16(10-15)12-23-27(20)2/h5-8,10-12,14H,3-4,9,13H2,1-2H3,(H,24,29)(H,25,26)/t14-/m0/s1
InChi Key
QGNDVASWIHEXCL-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    SGC-iMLLT is an inhibitor of the YEATS domain-containing proteins MLLT1 and MLLT3.1 It binds to the MLLT1 YEATS1 and MLLT3 YEATS3 domains (Kds = 129 and 77 nM, respectively).1 It is selective for YEATS1 and -3 over YEATS2 and -4 (IC50s = >10 µM), as well as a panel of 48 bromodomains at 50 µM. SGC-iMLLT inhibits the interaction of histone H3.3 with MLLT3 (IC50 = 400 nM in a reporter assay) and decreases expression of the tumorigenic genes MYC and DDN in MV-4-11 leukemia cells when used at a concentration of 1 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Moustakim, M., Christott, T., Monteiro, O.P., et al. Discovery of an MLLT1/3 YEATS domain chemical probe. Angew. Chem. Int. Ed. Engl. 57(50), 16302-16307 (2018).