18
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8839 |
ICCB280
|
Apoptosis; Others | Apoptosis; Others |
ICCB280 是一种 C/EBPα诱导剂,通过激活 C/EBPα 并影响其下游靶点,具有终末分化、增殖停滞和凋亡的抗白血病特性。 | |||
T3278 |
Piribedil
EU-4200,Trivastan,ET-495,Trivastal |
Dopamine Receptor; Histone Methyltransferase; Adrenergic Receptor | Chromatin/Epigenetic; GPCR/G Protein; Neuroscience |
Piribedil (Trivastan) 是多巴胺 D2受体激动剂,对 hα1A-肾上腺素受体也显示出拮抗作用。 | |||
T11766L |
Eltanexor
ONO-7706,KPT-8602,ATG-016 |
Others | Others |
Eltanexor (ONO-7706) 是一种具有口服活性的 exportin-1 (XPO1) 抑制剂。它具有有效的抗白血病活性。 Eltanexor 通过直接靶向 XPO1 抑制 XPO1 依赖性核输出 (EC50=60.9 nM)。 Eltanexor 在一组白血病细胞系中引起半胱天冬酶依赖性细胞凋亡。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T82583 |
Deoxyharringtonine
|
||
Deoxyharringtonine为从Cephalotaxus属植物中分离的生物碱,具备显著的抗白血病活性。 | |||
T39861 |
AS-85
|
||
AS-85 is a potent ASH1L histone methyltransferase inhibitor ( IC 50 =0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the K d value of 0.78 μM. | |||
T39482 |
Casein Kinase inhibitor A86
Casein Kinase inhibitor A86 |
||
Casein Kinase inhibitor A86 is a highly effective and orally bioavailable inhibitor of casein kinase 1α (CK1α). Additionally, it displays inhibitory actions towards CDK7 (TFIIH) and CDK9 (P-TEFb). Furthermore, Casein Kinase inhibitor A86 demonstrates the ability to induce apoptosis in leukemia cells, portraying substantial anti-leukemic effects. | |||
T35429 |
AC-4-130
|
||
AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ultimately leading to cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 exhibits notable anti-cancer properties and effectively suppresses abnormal STAT5 activity in acute myeloid leukemia (AML), making it a promising therapeutic option [1]. | |||
T67930 |
CWI1-2
|
Apoptosis | Apoptosis |
CWI1-2 是一种有效的 IGF2BP2 抑制剂,通过结合 IGF2BP2 抑制其与 m6A 修饰的靶转录物的相互作用。CWI1-2 具有抗白血病活性,可诱导细胞凋亡 (apoptosis)和分化。 | |||
T12240 |
nor-NOHA acetate
Nω-Hydroxy-nor-L-arginine acetate |
Apoptosis; Arginase | Apoptosis; Immunology/Inflammation |
nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) 是一种可逆的精氨酸酶抑制剂,具有抗白血病的作用,对内皮功能障碍、免疫抑制和代谢有效。在缺氧条件下,它可诱导 ARG2 表达细胞的凋亡。 | |||
T63332 |
BCR-ABL-IN-5
|
||
BCR-ABL-IN-5 是一种 Bcr-Abl (Breakpoint cluster region-Abelson) 激酶抑制剂,能够作用于 Bcr-AblWT (IC50: 0.014 μM)和 Bcr-AblT3151 (IC50: 0.45 μM),表现出一定的抗白血病细胞增殖作用。 | |||
T36978 | AS-99 TFA | ||
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1]. AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 TFA on any of the tested... | |||
T61098 |
RUNX1/ETO tetramerization-IN-1
|
||
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor that specifically targets NHR2 of RUNX1/ETO, effectively inhibiting the tetramerization process. With an EC50 value of 0.25 μM, this compound successfully restores gene expression that has been down-regulated by RUNX1/ETO. Furthermore, RUNX1/ETO tetramerization-IN-1 demonstrates promising anti-leukemic activity by inhibiting the proliferation of SKNO-1 cells dependent on RUNX1/ETO and significantly reducing RUNX1/ETO-associated tumor g... | |||
T73529 |
AS-99
|
||
AS-99 是首创的、有效的、选择性 ASH1L 组蛋白甲基转移酶抑制剂 (IC50= 0.79 µM,Kd= 0.89 µM),并具有抗白血病活性。AS-99 阻断细胞增殖,诱导细胞凋亡 (apoptosis) 和细胞分化,下调 MLL 融合靶基因,减少体内白血病负担。 | |||
T76893 | Lusvertikimab | ||
Lusvertikimab (OSE-127) 是一种人源化IL7R 单克隆抗体。Lusvertikimab 不会被靶细胞内化并阻止 IL7R 异二聚化和随后的下游信号传导。Lusvertikimab 具有抗白血病功效,具有用于 B 细胞前体急性淋巴细胞白血病 (BCP-ALL) 研究的潜力。 | |||
T82259 |
Grisnilimab setaritox
WT1-RTA |
||
Grisnilimab setaritox (WT1-RTA) 是抗人 T 细胞抗体 (anti-CD7) 与蓖麻毒素 A 链 (RTA) 的结合物。RTA 是一种质量为 30 kda 的肽,能迅速活化 60S 核糖体亚基。Grisnilimab setaritox 对体外 CEM (T 淋巴母细胞白血病) 细胞具有显著细胞毒性,ID50 为 53 pM,并在恒河猴白血病性脑膜炎模型中显示出疗效改善。 | |||
T83930 |
SJ 11646
|
||
SJ11646是一种高效的LCK(淋巴细胞特异性蛋白酪氨酸激酶)降解剂(PROTAC;DC50= 0.00838 pM)。该化合物由Dasatinib作为LCK配体,以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病(T-ALL)细胞株和初级白血病样本展现出细胞毒性。在体内,SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。 | |||
T78871 |
PLM-101
|
||
PLM-101是一种口服抗癌剂,针对FLT3和RET具有选择性抑制作用,有效抑制急性髓系白血病(AML)细胞。通过抑制RET,PLM-101促使FLT3的自噬降解,并且通过抑制PI3K和Ras/ERK信号通路来发挥其抗白血病的活性。在小鼠MV4-11侧翼异种移植模型中,PLM-101以口服剂量3及10 mg/kg显示出抗肿瘤效果,并且在同种异种移植小鼠模型中,剂量为40 mg/kg(口服)亦展现出明显的抗肿瘤功效。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN5888 |
Toddaculin
|
Others | Others |
Toddaculin 是一种天然香豆素,抑制过度的破骨细胞活性并增强成骨细胞分化和矿化。它可诱导白血病细胞分化和凋亡,具有抗炎活性。 | |||
T6S1315 |
Oroxylin A
千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether |
Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy | Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮,具有较强的抗癌作用。 | |||
T2S2215 |
Crebanine
|
Apoptosis; Others; Akt | Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling |
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。 |