MLL
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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抑制剂（6）
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7265 |
MM-102MM-102是一个高亲和力的多肽模拟的MLL1抑制剂，无细胞试验中IC50为0.4 μM。 |
(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.
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| S7816 |
MI-463MI-463是Menin-MLL interaction的有效抑制剂，IC50为15.3 nM。 |
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| S7817 |
MI-503MI-503是一种有效的、选择性的Menin-MLL抑制剂，IC50为14.7 nM。在人类MLL白血病细胞系中，具有显著的生长抑制效果（GI=250 nM-570 nM），但是在不具有MLL易位的人类白血病细胞中，效果甚微。 |
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| S7619 |
MI-3 (Menin-MLL Inhibitor)MI-3 (Menin-MLL Inhibitor)是一种强效的menin-MLL相互作用抑制剂，IC50为 648 nM。 |
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| S7618 |
MI-2 (Menin-MLL Inhibitor)MI-2 (Menin-MLL Inhibitor)是一种有效的menin-MLL相互作用抑制剂，IC50为446 nM。 |
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| S7815 |
MI-136MI-136抑制DHT所诱导的雄激素受体(AR)靶向基因的表达。 |
