Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6057 |
URMC-099
|
ROCK; MLK; VEGFR; SGK; DNA Alkylation; Trk receptor; c-Met/HGFR; LRRK2; MEK; IGF-1R; Syk; Bcr-Abl; CDK; Src; Aurora Kinase; Autophagy | Angiogenesis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
URMC-099 是一种具有优异的血脑屏障穿透性的,可口服的混合谱系激酶 3 抑制剂,IC50为14 nM。 | |||
T11520 |
GW806742X
|
MLK; VEGFR | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
GW806742X 是ATP 模拟物,是MLKL 抑制剂,可结合 MLKL 假激酶结构域,Kd 值为 9.3μM。它对VEGFR2的IC50为 2 nM,延缓 MLKL 膜移位并抑制坏死。 | |||
T6904 |
Necrosulfonamide
(E)-Necrosulfonamide |
MLK | MAPK |
Necrosulfonamide ((E)-Necrosulfonamide) 是一种坏死性凋亡抑制剂,通过选择性靶向(MLKL),可阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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 . | |||
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. | |||
T24471 | MIV-6 | ||
MIV-6 is an inhibitor of the menin-mixed lineage leukemia interaction. | |||
T17010 |
TC13172
|
Others | Others |
TC13172 is an inhibitor of mixed lineage kinase domain-like protein (EC50: 2 nM for HT-29 cells). | |||
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. | |||
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。 | |||
T39102 |
MLK-IN-1
|
||
MLK-IN-1 (US20140256733A1, compound 68) is a highly potent and selective inhibitor of mixed lineage kinase 3 (MLK-3). It exhibits excellent brain penetration and specifically targets MLK-3. | |||
T79731 |
MLKL-IN-6
|
Necroptosis | Apoptosis |
MLKL-IN-6(compound P28)是一种针对Mixed Lineage Kinase domain-like(MLKL)的混合谱系激酶抑制剂,具有抗纤维化的潜力。它能够抑制MLKL的磷酸化和寡聚化,从而抑制细胞坏死、免疫细胞死亡,并减少粘附因子的表达。MLKL-IN-6展现出低细胞毒性,并可抑制肝星状细胞的激活,从而降低肝纤维化标志物的水平。 | |||
T70593 |
GW-841819X
|
||
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia. Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic readers". BET bromodomains have emerged as promising drug targets for treatment of cancers | |||
T28630 |
RX-37
RX37 |
||
RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell growth in human acute leukemia cell | |||
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. | |||
T69014 |
Sekikaic Acid
|
||
Sekikaic acid is a phenolic lichen metabolite that has been found in H. obscurata and has diverse biological activities. It scavenges superoxide and DPPH radicals in cell-free assays when used at a concentration of 0.5 µM. Sekikaic acid is active against the rg recombinant strain of respiratory syncytial virus (RSV; IC50 = 5.69 µg/ml). It inhibits the protein-protein interaction between mixed lineage leukemia 1 (MLL1) and the GACKIX domain of CREB-binding protein (CBP; IC50 = 34 µM). | |||
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. | |||
T74681 | NecroIr2 | ||
NecroIr2 是一种铱 (III) 复合物,是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr2 选择性积累在线粒体中,导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr2 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL),调节CDK4表达。 | |||
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。 | |||
T74680 | NecroIr1 | ||
NecroIr1 是一种铱 (III) 复合物,是顺铂 (Cisplatin) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr1 选择性积累在线粒体中,导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr1 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL),调节CDK4表达。 | |||
T36574 |
GW841819X
GW841819X |
||
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70... |