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14

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6721 Vinblastine

Microtubule Associated; AChR Cytoskeletal Signaling; Neuroscience
Vinblastine 抑制微管形成并抑制 nAChR 活性,IC50 为 8.9 μM,用于治疗某些类型的癌症。
T18330 MC-Val-Cit-PAB-vinblastine

Others Others
MC-Val-Cit-PAB-vinblastine is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), featuring vinblastine (a microtubule protein inhibitor) connected through the MC-Val-Cit-PAB ADC linker.
T29434 4-Desacetylvinblastine hydrazide

DAVLBH,Deacetylvinblastine hydrazide,Desacetylvinblastine hydrazide

Deacetylvinblastine hydrazide, a cytotoxic vinca alkaloid often conjugated with folic acid to produce EC145, a novel folate-receptor targeted agent.
T10772 Cevipabulin

TTI-237

Microtubule Associated Cytoskeletal Signaling
Cevipabulin (TTI-237) 是一种微管活性的、口服有效的抗肿瘤化合物,可抑制 [3H] 长春碱与微管蛋白的结合,对人癌细胞的 IC50 值为 18-40 nM。
T10772L Cevipabulin fumarate

TTI-237 fumarate

Others Others
Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).
T17727 CCK2R Ligand-Linker Conjugates 1

Others Others
CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].
T13672 EC0489

Others Others
EC0489, Small molecule-drug conjugate (SMDC) ,a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor.
T26413 A 30312

A-30312,A30312

A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.
T21317 Avanbulin

BAL27862,BAL-27862,BAL 27862

Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range
T36856 UA 62784

Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 |Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cauti...
T25025 ALB-109564 dihydrochloride

ALB-109564 dihydrochloride 是长春碱生物碱的半合成衍生物,是一种微管蛋白抑制剂和抗肿瘤药物。它与微管蛋白单体结合并抑制微管的形成,导致有丝分裂纺锤体组装的破坏和肿瘤细胞停滞在细胞周期的G2/M 期。
T35616 Migrastatin

Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mam...
T38011 C2 Adamantanyl Globotriaosylceramide (d18:1/2:0)

C2 Adamantanyl globotriaosylceramide (AdaGb3) is a bioactive sphingolipid and water-soluble form of globotriaosylceramide that contains an adamantanyl group in place of the fatty acyl chain. It inhibits Vero toxin binding to globotriaosylceramide in an ELISA assay when used at a concentration of 10 μM. AdaGb3 decreases cell surface expression of P-glycoprotein (P-gp) and reduces efflux of rhodamine 123 in MDCK cells. It also increases apical-to-basal transport of vinblastine in human intestinal ...
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...

化合物

Vinblastine
Cat.No: T6721
Synonym:
Target: Microtubule Associated, AChR
MC-Val-Cit-PAB-vinblastine
Cat.No: T18330
Synonym:
Target: Others
4-Desacetylvinblastine hydrazide
Cat.No: T29434
Synonym: DAVLBH,Deacetylvinblastine hydrazide,Desacetylvinblastine hydrazide
Target:
Cevipabulin
Cat.No: T10772
Synonym: TTI-237
Target: Microtubule Associated
Cevipabulin fumarate
Cat.No: T10772L
Synonym: TTI-237 fumarate
Target: Others
CCK2R Ligand-Linker Conjugates 1
Cat.No: T17727
Synonym:
Target: Others
EC0489
Cat.No: T13672
Synonym:
Target: Others
A 30312
Cat.No: T26413
Synonym: A-30312,A30312
Target:
Avanbulin
Cat.No: T21317
Synonym: BAL27862,BAL-27862,BAL 27862
Target:
UA 62784
Cat.No: T36856
Synonym:
Target:
ALB-109564 dihydrochloride
Cat.No: T25025
Synonym:
Target:
Migrastatin
Cat.No: T35616
Synonym:
Target:
C2 Adamantanyl Globotriaosylceramide (d18:1/2:0)
Cat.No: T38011
Synonym:
Target:
PC-046
Cat.No: T71252
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T1668 Vinblastine sulfate

硫酸长春碱,NSC49842,Vincaleukoblastine sulfate salt

Microtubule Associated; AChR; Autophagy Autophagy; Cytoskeletal Signaling; Neuroscience
Vinblastine sulfate (Vincaleukoblastine sulfate salt) 是对各种癌症类型有细胞毒性的生物碱。 它可以抑制微管的形成,也可以抑制 nAChR,IC50值为8.9 μM。
T22455 Vindesine sulfate

DVA,Desacetylvinblastine amide,硫酸长春地辛,DAVA,Desacetyl Vinblastine amide,VDS

Others Others
Vindesine sulfate (Desacetyl Vinblastine amide) 是一种长春花生物碱,它是长春碱的合成衍生物,与有丝分裂纺锤体的微管蛋白结合,导致微管结晶和有丝分裂停滞或细胞死亡。
T12540 Pristinamycin IA

Mikamycin IA,普利霉素IA,Mikamycin B

Others; Antibiotic; P-gp Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Others
Pristinamycin IA (Mikamycin B) 是 P-糖蛋白的底物,也是一种环肽类大环内酯抗生素。
T3022 Anhydrovinblastine

脱水长春碱,3',4'-Anhydrovinblastine

Others Others
3',4'-Anhydrovinblastine (3',4'-Anhydrovinblastine) 是一种提取自Catharanthus roseus 叶片的单萜吲哚生物碱。
TN4695 Odorine

Others Others
Odorine has potent anti-carcinogenic effect by inhibiting both the initiation and promotion stages of two-stage skin carcinogenesis. It was found to inhibit the growth of the vinblastine-resistant KB cells by enhancing the anticancer activity of vinblastine.
TN5153 Torilin

MMP; ERK; IκB/IKK; p38 MAPK; NF-κB; Tyrosinase; Reductase; DNA/RNA Synthesis; JNK Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Endocrinology/Hormones; MAPK; Metabolism; NF-κB; Proteases/Proteasome
Torilin 是一种睾酮5α还原酶抑制剂,它(IC50=31.7+/-4.23μM)对5α还原酶的抑制作用强于α-亚麻酸(IC50=160.3+/-24.62μM),但弱于非那雄胺(IC50=0.38+/-0.06μM)。Torilin 具有免疫调节、肝脏保护和抗炎特性,它通过限制 TAK1介导的 MAP 激酶和 NF-βB 活化来抑制炎症,它可以减轻关节炎的严重程度,改变 dLN 或关节中的白细胞活化,并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的 B16黑色素瘤细胞中的黑色素生成,IC(50)值为25μM。Torilin 对枯草芽孢杆菌 ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin 在体内和体外都具有强大的抗血管生成活性,它可能通过抑制肿瘤侵袭来抑制肿瘤发生,逆转癌细胞的多药耐药性,它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药 KB-V1和 MCF7/ADR 细胞的细胞毒性。

天然产物

Vinblastine sulfate
Cat.No: T1668
Synonym: 硫酸长春碱,NSC49842,Vincaleukoblastine sulfate salt
Target: Microtubule Associated, AChR, Autophagy
Vindesine sulfate
Cat.No: T22455
Synonym: DVA,Desacetylvinblastine amide,硫酸长春地辛,DAVA,Desacetyl Vinblastine amide,VDS
Target: Others
Pristinamycin IA
Cat.No: T12540
Synonym: Mikamycin IA,普利霉素IA,Mikamycin B
Target: Others, Antibiotic, P-gp
Anhydrovinblastine
Cat.No: T3022
Synonym: 脱水长春碱,3',4'-Anhydrovinblastine
Target: Others
Odorine
Cat.No: TN4695
Synonym:
Target: Others
Torilin
Cat.No: TN5153
Synonym:
Target: MMP, ERK, IκB/IKK, p38 MAPK, NF-κB, Tyrosinase, Reductase, DNA/RNA Synthesis, JNK
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