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AB287022

MM-102 (HMTase Inhibitor IX)

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MW 669.8 Da, Purity >98%. MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM). It has been shown to block MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis. WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.

Key facts

CAS number

1417329-24-8

Purity

>98%

Form

Solid

form

Molecular weight

669.8 Da

Molecular formula

C<sub>3</sub><sub>5</sub>H<sub>4</sub><sub>9</sub>F<sub>2</sub>N<sub>7</sub>O<sub>4</sub>

PubChem

54766613

Nature

Synthetic

Solubility

Soluble in DMSO to >25 mM

Biochemical name

HMTase Inhibitor IX

Biological description

MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM). It has been shown to block MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis. WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.

Canonical smiles

CCC(CC)(C(=O)NC(CCCN=C(N)N)C(=O)NC1(CCCC1)C(=O)NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)NC(=O)C(C)C

Isomeric smiles

CCC(CC)(C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC1(CCCC1)C(=O)NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)NC(=O)C(C)C

InChi

InChI=1S/C35H49F2N7O4/c1-5-34(6-2,43-29(45)22(3)4)31(47)41-27(10-9-21-40-33(38)39)30(46)44-35(19-7-8-20-35)32(48)42-28(23-11-15-25(36)16-12-23)24-13-17-26(37)18-14-24/h11-18,22,27-28H,5-10,19-21H2,1-4H3,(H,41,47)(H,42,48)(H,43,45)(H,44,46)(H4,38,39,40)/t27-/m0/s1

InChiKey

RZKSQRIPRKWVBU-MHZLTWQESA-N

IUPAC Name

N-[bis(4-fluorophenyl)methyl]-1-[[(2S)-5-(diaminomethylideneamino)-2-[[2-ethyl-2-(2-methylpropanoylamino)butanoyl]amino]pentanoyl]amino]cyclopentane-1-carboxamide

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Complementary Products

Biochemicals

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Proteins & Peptides

AB268799

Recombinant human KMT2A / MLL protein (Active)

Functional Studies - Recombinant human KMT2A / MLL protein (Active) (AB268799)

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Primary Antibodies

AB32400

Anti-KMT2A / MLL antibody [mmN4.4]

BOND RX™ Validated|Trial Size

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-KMT2A / MLL antibody [mmN4.4] (AB32400)

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Primary Antibodies

AB239350

Anti-KMT3A / HYPB / HIF-1 antibody [EPR20927-67]

RabMAb|Recombinant|KO Validated|Trial Size

Western blot - Anti-KMT3A / HYPB / HIF-1 antibody [EPR20927-67] (AB239350)

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2364 MM-102. B2364-25 is the same size as the 25 mg size of ab287022.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

KMT2A also known as MLL (Mixed-Lineage Leukemia) is a lysine methyltransferase enzyme with a molecular mass around 431 kDa. This protein exists within the nucleus where it performs epigenetic regulation. KMT2A methylates lysine 4 on histone H3 promoting transcriptional activation. It is ubiquitously expressed in various tissues signaled to act within regions essential for cellular differentiation and development.
Biological function summary

KMT2A functions within a multi-protein complex often referred to as a histone methyltransferase complex. This includes core components like RbBP5 WDR5 and ASH2L. These components stabilize KMT2A and aid its enzymatic activity. KMT2A's role in chromatin remodeling is essential for the regulation of critical genes including Hox gene clusters which play a part in shaping body patterning during development.

Pathways

KMT2A's function is integrated within the epigenetic regulation and cell cycle control pathways. It interacts closely with proteins like Menin and LEDGF assisting in regulating the transcription of homeotic genes. KMT2A’s methylation activity also plays a role in DNA repair mechanisms underlining pathways that ensure genomic stability.

KMT2A is notably associated with acute leukemia specifically acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). Chromosomal translocations involving KMT2A lead to fusion proteins that disrupt normal gene regulation promoting uncontrolled proliferation. This protein has functional connections to other leukemia-associated proteins like AF4 and ENL which form part of aberrant fusion proteins in leukemias.
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Product protocols

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