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Search Results for " destabilizing "

12

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T74166	Microtubule destabilizing agent-1
	Microtubule destabilizing agent-1 (Compound 12b)为基于异羟肟酸的微管去稳定剂(MDA)。该化合物表现出良好的代谢稳定性、高生物利用度及有效的抗肿瘤活性。
T22661	CHM-1	Apoptosis; Others; Microtubule Associated	Apoptosis; Cytoskeletal Signaling; Others
	CHM-1 是细胞凋亡的诱导剂，通过激活 Cdc2 激酶活性在人肝细胞癌中显示出有效的抗肿瘤能力。 CHM-1 在体外和体内抑制微管蛋白聚合。
T13945	Tubulysin	Others	Others
	Tubulysin family are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, and are potent microtubule destabilizing agents.
T24788	Shield-2
	Shield-2 is a potent FKBP-derived destabilizing domain stabilizing ligand.
T34102	Podoverine A
	Podoverine A is a microtubule destabilizing natural product from the Podophyllum species.
T32147	IMC-76 NSC-59276,IMC 76,NSC 59276,NSC59276
	IMC-76 is a BCL2 i-motif-interactive compound that can act by destabilizing or unfolding the i-motif.
T27052	CMP3a CMP-3a,CMP 3a
	CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase E
T13937	Tubulysin B	Others	Others
	Tubulysin B is an agent of potent microtubule destabilizing and highly cytotoxic peptide isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis.
T4620	Siramesine 西拉美新,Lu 28-179	Sigma receptor	GPCR/G Protein
	Siramesine (Lu 28-179) 是sigma-2受体激动剂，通过线粒体的不稳定溶酶体触发细胞死亡，有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力，IC50为 0.12 nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍，IC50为 17 nM。
T68686	DAP-81
	DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations.
T71252	PC-046
	PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with di...
T74844	Antiproliferative agent-23
	Antiproliferative agent-23，一种微管去稳定剂(MDA)，通过扰乱微管蛋白-微管系统来发挥作用。该化合物通过降低Bcl-2蛋白水平、提高Bax和Cyt c蛋白水平以及激活半胱天冬酶级联反应和线粒体依赖途径来诱导细胞凋亡。此外，Antiproliferative agent-23还能在A549/CDDP细胞（顺铂耐药癌细胞系）中通过PERK/ATF4/CHOP信号通路激活ROS介导的内质网应激，展现出抗肿瘤活性。

化合物

Microtubule destabilizing agent-1

Cat.No: T74166

Cat.No: T22661

Target: Apoptosis, Others, Microtubule Associated

Cat.No: T13945

Target: Others

Cat.No: T24788

Cat.No: T34102

Cat.No: T32147

Synonym: NSC-59276,IMC 76,NSC 59276,NSC59276

Cat.No: T27052

Synonym: CMP-3a,CMP 3a

Cat.No: T13937

Target: Others

Cat.No: T4620

Synonym: 西拉美新,Lu 28-179

Target: Sigma receptor

Cat.No: T68686

Cat.No: T71252

Antiproliferative agent-23

Cat.No: T74844

Cat. No.	Product Name	Target	Signaling Pathways
T6272	Fosbretabulin Disodium Combretastatin A4 Phosphate,CA 4DP,CA 4P,福他布林,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Fosbretabulin Disodium (CA 4P) 是一种微管蛋白去稳定剂，是 Combretastatin A4 前药，可选择性靶向内皮细胞，诱导新生肿瘤新血管消退，减少肿瘤血流量并引起中央肿瘤坏死。
T3S0209	Vincristine	ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR	Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling
	Vincristine 与微管蛋白结合并抑制微管的形成，从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂，用于研究治疗血液系统癌症，如白血病和淋巴瘤以及儿童肉瘤的相关研究。

天然产物

Fosbretabulin Disodium

Cat.No: T6272

Synonym: Combretastatin A4 Phosphate,CA 4DP,CA 4P,福他布林,Combretastatin A4 disodium phosphate,Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium

Target: Apoptosis, Microtubule Associated

Cat.No: T3S0209

Target: ERK, p38 MAPK, NF-κB, Akt, JNK, mTOR

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