- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S7265||MM-102||100 mg/mL||100 mg/mL||100 mg/mL|
|S7816||MI-463||<1 mg/mL||96 mg/mL||22 mg/mL|
|S7817||MI-503||<1 mg/mL||100 mg/mL||15 mg/mL|
|S7619||MI-3 (Menin-MLL Inhibitor)||<1 mg/mL||19 mg/mL||19 mg/mL|
|S7618||MI-2 (Menin-MLL Inhibitor)||<1 mg/mL||75 mg/mL||75 mg/mL|
|S7815||MI-136||<1 mg/mL||94 mg/mL||94 mg/mL|
- MLL Inhibitors (6)
|Catalog No.||Information||Product Use Citations||Product Validations|
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
(D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey's test for multiple comparisons was performed. *, P < 10−2; ****, P < 10−5; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. *, P < 10−2; **, P < 10−3; ***, P < 10−4; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.
MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.
MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.