Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2649 |
Menin-MLL inhibitor MI-2
Menin-MLL Inhibitor,MI2,MI-2,Menin-MLL inhibitor 2,MI 2 |
Apoptosis; Epigenetic Reader Domain; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
Menin-MLL inhibitor MI-2 (MI2) 抑制Menin-MLL 相互作用,IC50为 446±28 nM。 | |||
T9399 |
Menin-MLL inhibitor 20
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
Menin-MLL inhibitor 20 是一种不可逆的menin-MLL 相互作用抑制剂,具有抗肿瘤活性。 | |||
T2643 |
MI-3
Menin-MLL Inhibitor,Menin-MLL inhibitor 3,MI 3 |
Apoptosis; Epigenetic Reader Domain; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
MI-3 (Menin-MLL Inhibitor)是一种有高亲和力的 menin-MLL 抑制剂,IC50值为 648 nM,Kd 值为 201 nM。 | |||
T69629 | M‑89 MLL inhibitor | ||
M‑89 is a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein−Protein Interaction (Kd = 1.4 nM; IC50 = 25nM). M-89 binds to menin with a Kd value of 1.4 nM and effectively engages cellular menin protein at low nanomolar concentrations. M-89 inhibits cell growth in the MV4;11 and MOLM-13 leukemia cell lines carrying MLL fusion with IC50 values of 25 and 55 nM, respectively, and demonstrates >100-fold selectivity over the HL-60 leukemia cell line lacking MLL fusion. | |||
T12002 |
Menin-MLL inhibitor 4
|
Others | Others |
Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction . | |||
T78151 |
Bleximenib oxalate
Menin-MLL inhibitor 24 oxalate |
Epigenetic Reader Domain | Chromatin/Epigenetic |
Bleximenib (Menin-MLL inhibitor 24) oxalate 是一种用于癌症研究的menin-mixed-lineage leukemia 1(menin-MLL)抑制剂。 | |||
T3082 |
SGC0946
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂,IC50值为0.3nM,可选择性地杀死混合谱系白血病细胞。 | |||
T72360 |
Menin-MLL inhibitor 26
|
||
Menin-MLL inhibitor 26 是一种 Menin-MLL 抑制剂。Menin-MLL inhibitor 26 也是一个活性参照物。 Menin-MLL inhibitor 26 可以抑制细胞生长。Menin-MLL inhibitor 26 可用于白血病的研究。 | |||
T79117 |
Menin-MLL inhibitor 27
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
Menin-MLL inhibitor 27 是一种化合物,它能有效抑制Menin-MLL之间的相互作用,对于研究癌症具有潜在价值,尤其是在急性骨髓性白血病方面。 | |||
T79737 |
Menin-MLL inhibitor 29
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
Menin-MLL inhibitor 29(Compound C1)是一种选择性Menin-MLLPPI抑制剂。该化合物与Menin紧密结合,具有138 nM的KD值,并以46 nM的IC50值明显抑制Menin与MBM1(Menin结合motif 1)的相互作用。在体外条件下,Menin-MLL inhibitor 29对HepG2和Hep3B肝癌细胞系表现出抑制增殖的作用(IC50s分别为0.31 μM和0.71 μM),也能有效抑制肿瘤生长。 | |||
T72135 |
(1s,4s)-Menin-MLL inhibitor-23
|
||
(1s,4s)-Menin-MLL inhibitor-23 是Menin-MLL inhibitor-23 的对应异构体。Menin-MLL inhibitor-23 (Example 99A) 是一种menin-MLL 相互作用抑制剂。 | |||
T13336 |
VTP50469
|
Apoptosis; Epigenetic Reader Domain; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
VTP50469 是一种高选择性和口服活性的Menin-MLL 相互作用抑制剂,具有有效的抗白血病活性,Ki 为 104 pM。 | |||
T8838 |
CCI-007
|
Apoptosis; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
CCI 007 是一种具有细胞毒性的选择性白血病抑制剂,在MLL 重排的敏感系婴幼儿白血病细胞中,IC50为2.5-6.2 μM。 | |||
T12943 |
SNDX-5613
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
SNDX-5613 是一种 Menin-MLL 特异性抑制剂,Ki 为 0.149 nM,IC50 为 10 在 20 nM 之间,可用于 MLL 基因重排的急性白血病研究。 | |||
T6916 |
OICR-9429
OICR 9429 |
Histone Methyltransferase; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
OICR-9429 是一个新颖的相互作用的小分子Wdr5-MLL 拮抗剂,IC50是 5 uM,在体外抑制急性髓性白血病细胞。 | |||
T28036 |
MI-2-2
MI22,MI 2 2 |
Histone Methyltransferase | Chromatin/Epigenetic |
MI-2-2 是一种抑制 menin 和 MLL 之间二价蛋白质-蛋白质相互作用的抑制剂,IC50 为 46 nM。 MI-2-2 与 menin 结合,Kd 为 22 nM。 | |||
T69628 |
Iptacopan hydrochloride hydrate
|
||
Iptacopan hydrochloride hydrate is a highly potent and highly selective factor B inhibitor. | |||
T12886 |
SGC-iMLLT
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC-iMLLT 是一种选择性的MLLT1/3-组蛋白相互作用抑制剂,IC50值为 0.26 μM,也是化学探针。它对 MLLT1 YEATS 域 (YD) 和 MLLT3 YD (AF9/YEATS3) 具有高结合力,Kd 值分别为 0.129 和 0.077 μM。 | |||
T69581 |
NVS MLLT-1
|
||
NVS-MLLT-1 is a selective inhibitor of YEATS domain of MLLT1 and MLLT3. | |||
TQ0069 |
MI-503
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
MI-503 是一种高效且可口服的 menin-mLL 相互作用抑制剂。 | |||
T16072 |
MI-538
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
MI-538是一种menin 和MLL 融合蛋白相互作用的抑制剂,IC50值为 21 nM。 | |||
T11925 |
M‑89
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
M-89 可抑制 Menin-MLL 蛋白之间的相互作用,有研究混合谱系白血病的潜力。它是一种强特异性 menin 抑制剂,结合到 menin 的Kd 值为 1.4 nM。 | |||
TQ0058 |
MI-463
|
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
MI-463 是一种有口服活性的menin-mLL 相互作用的高效小分子抑制剂,IC50为15.3 nM。 | |||
T10706 |
CCI-006
|
Mitochondrial Metabolism | Metabolism |
CCI-006 是一种 MLL 重排白血病细胞的选择性抑制剂和化学增敏剂。 它能够抑制线粒体呼吸,造成 MLL-r 白血病细胞亚群中无法克服的线粒体去极化和促凋亡未折叠蛋白反应。 | |||
T77339 |
BRD4-IN-4
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
BRD4-IN-4 是一种具有选择性的 BRD4 抑制剂 ,对 BRD4 的IC50值为 6.83 μM。BRD4-IN-4 选择性抑制 MV4-11 细胞系增殖并将细胞阻滞在 G1 期。BRD4-IN-4可用于研究 MLL 白血病。 | |||
T8768 |
MM-102 TFA
HMTase Inhibitor IX TFA |
Histone Methyltransferase | Chromatin/Epigenetic |
MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂,在 WDR5 结合检测中,IC50为 2.4 nM,Ki 小于 1 nM。 | |||
T4247 |
I-CBP112 hydrochloride
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
I-CBP112 hydrochloride 是含溴结构域转录因子的选择性抑制剂,靶向 CBP/p300 溴结构域。在体内外,它以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜力,还增加 BET 溴结构域抑制剂 JQ1 以及阿霉素的细胞毒活性。 | |||
T6889 |
MI-136
|
Apoptosis; Epigenetic Reader Domain; Androgen Receptor | Apoptosis; Chromatin/Epigenetic; Endocrinology/Hormones |
MI136 是 menin-MLL(PPI) 蛋白互作的抑制剂,其 IC50值为31 nM,Kd 值为23.6 nM。它可抑制 DHT 诱导的雄激素受体 (AR) 靶基因的表达,有用于去势抵抗性肿瘤的潜能。 | |||
T6333 |
MM-102
MM102,HMTase Inhibitor IX |
Histone Methyltransferase | Chromatin/Epigenetic |
MM-102 (HMTase Inhibitor IX) 是一种有效的 WDR5/MLL 相互作用抑制剂,在 WDR5 结合检测中,IC50为 2.4 nM,Ki 小于 1 nM。 | |||
T39937 |
M-808
|
||
M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM. | |||
T27134 |
DCYM21
DC YM 21,DC-YM21,DCYM-21,DC_YM21,DC YM21 |
||
DCYM21 is an inhibitor of menin-MLL interaction. DCYM21 demonstrates potent and selective blockage of proliferation and induces both cell cycle arrest and differentiation of leukemia cells harboring MLL translocations. | |||
T15831 |
M-525
|
Others | Others |
M-525 binds to menin (IC50: 3 nM) and achieves low nanomolar potencies in cell growth inhibition and in the suppression of MLL regulated gene expression in MLL leukemia cells. M-525 is a first-in-class, highly potent, irreversible, and covalent menin-MLL | |||
T69624 |
TC-5115
|
||
TC-5115 is a potent inhibitor of MLL methyltransferase with IC50 value of 16 nM. TC-5115 may lead to the development of a new therapy for the treatment of human MLL leukemia. The mixed-lineage leukemia (MLL) protein, also known as MLL1, is a lysine methyltransferase specifically responsible for methylation of histone 3 lysine 4. MLL has been pursued as an attractive therapeutic target for the treatment of acute leukemia carrying the MLL fusion gene or MLL leukemia. | |||
T61735 |
MI-1
|
||
MI-1 抑制 Menin-MLL 相互作用,IC50为 1.9 μM。 | |||
T24472 |
MIV-6R
MIV6R,VU05163101,VU0516310-1,VU0516310 1,MIV 6R |
||
MIV-6R is an inhibitor of the menin- MLL interaction that acts by demonstrating strong and selective effects in MLL leukemia cells and validating specific mechanisms of action. | |||
T12091L |
MM-589 TFA
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction. | |||
T22978 | MI-2 (hydrochloride) | Others | Others |
MI-2 (Menin-MLL Inhibitor) is an effective menin-MLL interaction inhibitor (IC50: 446 ± 28 nM). | |||
T12290 |
OICR-0547
|
Others | Others |
OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule Wdr5-MLL interaction antagonist. | |||
T24484 |
ML399
VU-0516340,VU 0516340,ML-399,VU0516340,ML 399 |
||
ML399 is the menin-- MLL interaction inhibitor that acts by demonstrating strong and selective effects in MLL leukemia cells and validating specific mechanism of action. | |||
T39585 |
Ziftomenib
KO-539 |
Histone Methyltransferase | Chromatin/Epigenetic |
Ziftomenib (KO-539) 是一种具有抗肿瘤活性的 menin-MLL 相互作用抑制剂,可以用于研究白血病。 | |||
T39938 |
M-1211
|
||
M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression. | |||
T24463 |
MI-1481
MI 1481 |
||
MI-1481 is an effective MML1 inhibitor (IC50: 3.6 nM). MI-1481 showed very potent inhibition of the menin-MLL1 interaction (IC50: 3.6 nM). MI-1481 also demonstrates pronounced activity in MLL leukemia cells and in vivo in MLL leukemia models. | |||
T82598 |
DDO-2213
|
||
DDO-2213是一口服有效的WDR5-MLL1抑制剂,具有29 nM的IC50和72.9 nM的Kd值针对WDR5蛋白。该化合物对MLL组蛋白甲基转移酶活性及MLL易位细胞增殖具有选择性抑制作用,可用于研究MLL融合型白血病。 | |||
TP2115 |
SAH-EZH2
|
||
EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line. | |||
T12091 |
MM-589
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction. | |||
T13336L |
VTP50469 fumarate
|
Others | Others |
VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity. | |||
T28269 |
ORY-1001 free base
RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016 |
||
ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a | |||
T72239 |
DDO-2093 dihydrochloride
|
||
DDO-2093 dihydrochloride 是一种有效的MLL1和WDR5蛋白-蛋白相互作用抑制剂 (IC50=8.6 nM ; Kd=11.6 nM),具有抗肿瘤活性。DDO-2093 dihydrochloride 选择性抑制 MLL 复合物的催化活性。 | |||
T62915 |
Dot1L-IN-7
|
||
Dot1L-IN-7 (compound 25) 是一种选择性的、有效的端粒沉默 1 样蛋白 (DOT1L) 抑制剂 (IC50: 1.0 μM)。Dot1L-IN-7 能够选择性地杀死 MLL-AF9,且不影响 E2A-HLF 细胞的生长。 | |||
T69846 |
VTP50469 mesylate
|
||
VTP-50469 is a novel, potent, selective, orally-available MeninMLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLLrearrangements and NPM1c+ mutations. |