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Search Results for " leukemic "

42

抑制剂 & 化合物

9

天然产物

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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。
T6641	Rilmenidine Phosphate	Apoptosis; Adrenergic Receptor; Autophagy; Imidazoline Receptor	Apoptosis; Autophagy; GPCR/G Protein; Neuroscience
	Rilmenidine phosphate 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体激动剂。它可调节白血病细胞增殖，刺激促凋亡蛋白 Bax，从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。它可通过减少交感神经过度活跃而发挥中枢作用，并通过抑制 Na+/H+反向转运而在肾脏中发挥作用。
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。
T12575	Unesbulin PTC596	Apoptosis; BMI-1	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 抑制剂。它在急性髓细胞白血病细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡，具有抗白血病作用。
T8531	m-3M3FBS 2,4,6-三甲基-N-[3-(三氟甲基)苯基]苯磺酰胺	Apoptosis; Phospholipase	Apoptosis; Metabolism
	m-3M3FBS 是一种有效的磷脂酶C 激活剂，刺激人中性粒细胞产生超氧物，上调细胞内钙离子浓度，刺激多种细胞产生磷酸肌醇。它诱导单核细胞白血病细胞凋亡。
T4215	TCS-PIM-1-4a 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-4a	Apoptosis; Pim	Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling
	TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂，可通过激活 AMPK 来阻断 mTORC1的活性。它可杀死多种髓样和淋巴样细胞系，IC50值为 0.8 μM 至 40 μM。
T15337	Forodesine 呋咯地辛,BCX-1777,Immucillin-H	Others	Others
	Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine is an orally active inhibitor of purine nucleoside phosphorylase (IC50s: 0.48 to 1.57 nM for human, mouse, rat, monkey, and dog PNP). It could induce apoptosis in leukemic cells b
T14550	BETd-260 ZBC 260	Epigenetic Reader Domain	Chromatin/Epigenetic
	BETd-260是一种 PROTAC，由 Cereblon 配体和 BET 配体相连，对白血病细胞株 BRD4蛋白的抑制作用。
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。
T39584	MI-3454
	MI-3454 is a highly potent, orally active, and selective inhibitor of the interaction between menin and MLL1, with an IC50 of 0.51 nM. This compound effectively inhibits the proliferation of leukemic cells and promotes their differentiation, leading to the regression or complete remission of leukemia in mouse models featuring MLL1 rearrangements or NPM1 mutations. This remarkable therapeutic effect is achieved through the downregulation of key genes involved in the development of leukemia.
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。
T9428	HM43239	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	HM43239 是一种具有口服活性和选择性 FLT3抑制剂，IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其凋亡 (apoptosis)。
T68736	KU-0058948
	KU-0058948 is a poly (ADP-ribose) polymerase (PARP) inhibitor that induces cell cycle arrest and apoptosis of primary myeloid leukemic cells and myeloid leukemic cell lines in vitro.
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。
T38718	Cytarabine triphosphate Cytarabine triphosphate,Ara-CTP
	Cytarabine triphosphate (Ara-CTP), a competitive inhibitor of DNA synthesis and an active metabolite of Cytarabine, exhibits predictive potential for leukemic blasts' chemosensitivity to Cytarabine through intracellular levels.
T41205	3',3'-cGAMP sodium salt
	3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemic regression in Eμ-TCL1 mice.
T23975	Deacylcortivazol UNII-3JO09QT49F,DAC,NSC 325316
	Deacylcortivazol (DAC) is a potent glucocorticoid. When incubated with glucocorticoid-resistant mutants derived from the glucocorticoid-sensitive human leukemic cell line CEM-C7, DAC caused significant growth inhibition. The cytotoxicity of DAC at concent
T61858	HDAC8-IN-3
	HDAC8-IN-3 (compound P19) is a highly potent inhibitor of HDAC8, displaying an IC50 value of 9.3 μM and producing thermal stabilization. Moreover, HDAC8-IN-3 exhibits cytotoxicity and induces apoptosis specifically in leukemic cell lines [1].
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.
T22104	ML-291
	ML291 is a sufonamidebenzamide compound that induces the unfolded protein response (UPR) and overwhelms the adaptive capacity of UPR, resulting in apoptosis in various solid cancer models. It activates the PERK/eIF2a/CHOP apoptotic pathway of UPR and reduces leukemic cell burden [1].
T41062	HXR9
	HXR9 is a cell-permeable peptide that acts as a competitive antagonist of the HOX/PBX interaction. It effectively inhibits the binding between HOX proteins and the transcription factor PBX, specifically in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with a high expression of the HOXA/PBX3 genes, for instance, MLL-rearranged leukemic cells.
T11313	Forodesine hydrochloride BCX-1777 hydrochloride,Immucillin-H hydrochloride	Others	Others
	Forodesine hydrochloride (BCX-1777 hydrochloride), a potent inhibitor of human lymphocyte proliferation, effectively induces apoptosis in leukemic cells by elevating dGTP levels. This compound is an orally active, highly potent purine nucleoside phosphorylase (PNP) inhibitor, demonstrating IC50 values between 0.48 to 1.57 nM across human, mouse, rat, monkey, and dog PNP.
T38428	Alisertib sodium MLN 8237 sodium
	Alisertib sodium (MLN 8237) is a potent and specific inhibitor (IC50 = 1.2 nM) of Aurora A kinase, an enzyme involved in cell division. By binding to Aurora A kinase, Alisertib sodium disrupts the formation of the mitotic spindle and causes abnormal cell division. At the molecular level, it acts on the AKT/mTOR/AMPK/p38 pathway, leading to the induction of apoptosis and autophagy in leukemic cells. This compound exhibits significant antitumor activity.
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].
T61101	FLT3-IN-13
	FLT3-IN-13 (compound 20) is a highly effective inhibitor targeting both topoisomerase II and FLT3 proteins in leukemic cells. It exhibits potent activity against these targets, with IC50 values of 2.26 μM for both. Moreover, FLT3-IN-13 induces cell cycle arrest at the G2/M phase and promotes apoptosis. Notably, it displays considerable anticytotoxic activity, specifically against leukemia [1].
T78733	ZLD115
	ZLD115（化合物44）为FB23衍生的FTO抑制剂，作为抗白血病药物，对白血病细胞系展示抗增殖效果。
T76185	N-Myristoyl-Lys-Arg-Thr-Leu-Arg
	N-Myristoyl-Lys-Arg-Thr-Leu-Arg 是一种蛋白激酶 C (PKC) 抑制剂，其 IC50值为 75 μM。N-Myristoyl-Lys-Arg-Thr-Leu-Arg 抑制人白血病细胞系 Jurkat 中 IL-2受体的诱导和 IL-2的产生。
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...
T80737	ZG36
	ZG36是一种人类Caseinolytic protease P(ClpP)激动剂，具有非选择性地降解呼吸链复合物和减少线粒体DNA的能力，从而导致线粒体功能衰竭及白血病细胞死亡。此外，ZG36能够抑制异种移植小鼠模型中急性髓细胞性白血病的发展。
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。
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...
T71400	Quizartinib HCl
	Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 / STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell pro...
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。
T79133	UC-764864	E1/E2/E3 Enzyme	Ubiquitination
	UC-764864是一种UBE2N抑制剂，能够抑制其酶活性，并对白血病细胞中的UBE2N依赖性信号传导具有细胞毒性作用。此外，UC-764864还能阻断人AML细胞系中先天免疫和炎症相关底物的泛素化。
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。
T76213	HXR9 hydrochloride
	HXR9 hydrochloride 是一种针对 HOX/PBX 相互作用的细胞渗透性肽类竞争性拮抗剂。它通过阻碍 HOX 蛋白与 PBX，一个与旁系同源基因组 1 至 8 结合的第二转录因子，之间的相互作用来发挥作用。特别地，HXR9 hydrochloride 能够选择性抑制细胞增殖，并在表达 HOXA/PBX3 基因高水平的细胞中，如 MLL 重排的白血病细胞，促进细胞凋亡。
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。

化合物

Cat.No: T8839

Target: Apoptosis, Others

Rilmenidine Phosphate

Cat.No: T6641

Target: Apoptosis, Adrenergic Receptor, Autophagy, Imidazoline Receptor

Cat.No: T3278

Synonym: EU-4200,Trivastan,ET-495,Trivastal

Target: Dopamine Receptor, Histone Methyltransferase, Adrenergic Receptor

Cat.No: T12575

Synonym: PTC596

Target: Apoptosis, BMI-1

Cat.No: T8531

Synonym: 2,4,6-三甲基-N-[3-(三氟甲基)苯基]苯磺酰胺

Target: Apoptosis, Phospholipase

Cat.No: T4215

Synonym: 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-4a

Target: Apoptosis, Pim

Cat.No: T15337

Synonym: 呋咯地辛,BCX-1777,Immucillin-H

Target: Others

Cat.No: T14550

Synonym: ZBC 260

Target: Epigenetic Reader Domain

Cat.No: T11766L

Synonym: ONO-7706,KPT-8602,ATG-016

Target: Others

Cat.No: T39584

Cat.No: T64338

Synonym: AKI 603,AKI-603

Target: Aurora Kinase

Cat.No: T9428

Target: FLT

Cat.No: T68736

Deoxyharringtonine

Cat.No: T82583

Cytarabine triphosphate

Cat.No: T38718

Synonym: Cytarabine triphosphate,Ara-CTP

3',3'-cGAMP sodium salt

Cat.No: T41205

Deacylcortivazol

Cat.No: T23975

Synonym: UNII-3JO09QT49F,DAC,NSC 325316

Cat.No: T61858

Cat.No: T39861

Casein Kinase inhibitor A86

Cat.No: T39482

Synonym: Casein Kinase inhibitor A86

Cat.No: T22104

Cat.No: T41062

Forodesine hydrochloride

Cat.No: T11313

Synonym: BCX-1777 hydrochloride,Immucillin-H hydrochloride

Target: Others

Alisertib sodium

Cat.No: T38428

Synonym: MLN 8237 sodium

Cat.No: T35429

Cat.No: T61101

Cat.No: T78733

N-Myristoyl-Lys-Arg-Thr-Leu-Arg

Cat.No: T76185

Cat.No: T67930

Target: Apoptosis

nor-NOHA acetate

Cat.No: T12240

Synonym: Nω-Hydroxy-nor-L-arginine acetate

Target: Apoptosis, Arginase

Cat.No: T63332

Cat.No: T36978

Cat.No: T80737

Cat.No: T73529

RUNX1/ETO tetramerization-IN-1

Cat.No: T61098

Quizartinib HCl

Cat.No: T71400

Cat.No: T76893

Cat.No: T79133

Target: E1/E2/E3 Enzyme

Grisnilimab setaritox

Cat.No: T82259

Synonym: WT1-RTA

HXR9 hydrochloride

Cat.No: T76213

Cat.No: T83930

Cat.No: T78871

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。
T2S1040	Jolkinolide B	ERK; IL Receptor; BCL; p38 MAPK; TNF; NF-κB; Akt; Caspase; PI3K; JAK; JNK; STAT; mTOR	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Jolkinolide B 是一种从 Euphorbia fischeriana Steud 的根中分离出来的具有生物活性的二萜。 Jolkinolide B 诱导癌细胞凋亡。 Jolkinolide B 可用于预防和治疗骨溶解的研究。
TN2190	Scoulerine	Apoptosis; Beta-Secretase; BACE; Parasite	Apoptosis; Microbiology/Virology; Neuroscience
	Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖，阻止细胞周期，并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。
T7730	Aminopterin APGA,氨基蝶呤,4-Aminofolic acid	Antifolate	Cell Cycle/Checkpoint
	Aminopterin (4-Aminofolic acid) 是叶酸的 4-氨基衍生物，是叶酸拮抗剂，具有抗癌和免疫抑制活性，用于研究儿童白血病。它催化叶酸还原为四氢叶酸，竞争性抑制二氢叶酸还原酶，Ki 值为 3.7 pM。
TN2496	1,4-Anthraquinone	Others	Others
	1,4-Anthraquinone 是一种抗癌药物，在体外与柔红霉素相同纳摩尔范围内阻断核苷转运、抑制大分子合成、诱导 DNA 片段化并降低 L1210 白血病细胞的生长和活力。它被提议为一种用于高效液相色谱 (HPLC) 测定药物制剂中 N-乙酰半胱氨酸 (NAC) 和卡托普利 (CAP) 的新型柱前试剂。
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。
TN4799	Piptocarphin F	Others	Others
	Piptocarphin F shows strong cytotoxic activities against mouse lymphoid tumor cell line P388. It also shows cytotoxic activity (IC50 3.87-12.5 umol/L) against the human leukemic cell line HL-60.
T83561	(2S)-4'-Hydroxy-7-methoxyflavan
	(2S)-4'-Hydroxy-7-methoxyflavan是一种对人白血病Molt 4细胞展示显著细胞毒性的黄烷化合物。

天然产物

Cat.No: TN5888

Target: Others

Cat.No: T2S1040

Target: ERK, IL Receptor, BCL, p38 MAPK, TNF, NF-κB, Akt, Caspase, PI3K, JAK, JNK, STAT, mTOR

Cat.No: TN2190

Target: Apoptosis, Beta-Secretase, BACE, Parasite

Cat.No: T7730

Synonym: APGA,氨基蝶呤,4-Aminofolic acid

Target: Antifolate

1,4-Anthraquinone

Cat.No: TN2496

Target: Others

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Cat.No: TN4799

Target: Others

(2S)-4'-Hydroxy-7-methoxyflavan

Cat.No: T83561

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