Propyzamide - CAS:23950-58-5

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Propyzamide (Synonyms:肟菊草胺; Kerb; RH 315)

目录号 : KM32825 CAS No. : 23950-58-5 纯度 : ≥99%

Data Sheet 产品使用指南

Propyzamide (Kerb) 是一种口服有效的 β-tubulin 和 AHR 信号通路抑制剂。Propyzamide 在二聚体内界面结合 β-tubulin，破坏微管组装，导致有丝分裂阻滞和多极纺锤体形成。Propyzamide 增强 C/EBPβ 和 NF-κB 信号传导，促进致结肠炎性辅助性 T 细胞分化以及表达 interleukin-17/interferon gamma 的结肠 T 细胞。Propyzamide 可用于结肠炎、炎症性肠病和肝癌的研究。

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
10g		In-stock

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Other Forms of Rapamycin:

Propyzamide In-stock
BI-765423 In-stock
Crebankitug In-stock
Levilimab In-stock
Sarilumab In-stock

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生物活性

Propyzamide (Kerb) is an orally active inhibitor of β-tubulin and AHR signaling pathways. Propyzamide binds β-tubulin at the intradimer interface, disrupting microtubule assembly, leading to mitotic arrest and multipolar spindle formation. Propyzamide enhances C/EBPβ and NF-κB signaling, promoting colitogenic helper T cell differentiation and interleukin-17/interferon gamma-expressing colonic T cells. Propyzamide can be used in research on colitis, inflammatory bowel disease, and liver cancer.

IC₅₀&Target

β-Tubulin AhR NF-κB

体外研究

Propyzamide (2-10 µM) enhances Th1/Th17 differentiation in mouse naive CD4+T cells and human CD3+T cells in an NF - κ B-C/EBP β - dependent manner.
Propyzamide (20 μM; 48-72 h) blocked Vigna radiata root meristematic cells in the early stage (83.41% at 48 h); 73.26% at 72 hours) and disrupted spindle microtubules.
Propyzamide (100 μM; 6 days) inhibited Nicotiana tabcum cv. BY-2 cell division, with an inhibition rate of 53% in conductivity measurements.
Propyzamide (0.75 μM-0.1 M; 24 h) caused complete depolymerization of cortical microtubules and spindle microtubules in Nicotiana tabcum cv. BY-2 cells, and induced multipole spindle formation.

Propyzamide (2-10 µM) inhibits FICZ induced AHR target gene expression in human and mouse primary DCs and T cells.
Propyzamide (2-10 µM) enhances T cell activation and Th1/Th17 polarization in mouse and human DCs, dependent on C/EBP β.

Cell Viability Assay

Cell Line:	differentiated HepaRG cells
Concentration:	3.13, 6.25, 12.5, 25, 50 μM (PRO alone); 3.13, 6.25, 12.5, 25, 50 μM (combined with 0.6 μM MCs)
Incubation Time:	24 hours
Result:	Did not reduce cell viability at the highest tested concentration (50 μM). Mixtures of PRO (3.13-50 μM) with MCs (0.6 μM) reduced cell viability to approximately 80% at 50 μM PRO + 0.6 μM MCs.

Real Time qPCR

Cell Line:	differentiated HepaRG cells
Concentration:	3.13, 6.25, 12.5, 25, 50 μM
Incubation Time:	24 hours
Result:	Induced expression of all marker genes. Significant effects on CYP2B6 and CYP3A4 were found from 6.25 μM (BMDL 11.3 and 14.6 μM, respectively). At the highest tested concentration, expression was increased by 3.4-fold for CYP2B6 and 3.0-fold for CYP3A4. CYP1A2 and GPX2 appeared to increase in a concentration-dependent manner, but the effects were not significant.

体内研究

Propyzamide (100 mg/kg; gavage; 7-day exacerbation of anti-CD3 induced enteritis and T-cell driven small intestinal inflammation in mice.
Propyzamide (100 mg/kg; intraperitoneal injection for 3 days and/or gavage) does not induce intestinal inflammation or alter baseline intestinal immune cell populations in healthy mice.
Propyzamide (100 mg/kg; intraperitoneal injection for 3 days to pre sensitize TNBS; Subsequently, the TNBS induced colitis in mice was aggravated by amplifying the pro-inflammatory AHR-NF - κ B-C/EBP β signal through continuous gavage to TNBS rectum stimulation for 6 days.
Propyzamide (0.2-20 μM; in E3 medium; 24-72 hours) can amplify TNBS induced zebrafish intestinal inflammation, but does not cause inflammation in untreated juvenile fish.

Animal Model:	AB wild-type and lck:gfp (7 days post-fertilization larvae)
Dosage:	0.2, 1, 5, and 20 μM
Administration:	in E3 medium; co-administered with 25 μg/mL TNBS; 24-72 h starting at 7 d.p.f.
Result:	Boosted TNBS-induced intestinal inflammation in zebrafish, as indicated by intestinal scores and expression of pro-inflammatory genes. In TNBS-exposed zebrafish, Propyzamide at 20 μM was tested in combination with TNBS; quantification of intestinal GFP-positive T cells in lck:gfp zebrafish was performed. Did not induce intestinal inflammation in the absence of TNBS. AHR activation by FICZ or NOS inhibition partially interfered with the worsening of TNBS-induced colitis by Propyzamide.

分子式

C₁₂H₁₁Cl₂NO

分子量

256.13

CAS号

23950-58-5

中文名称

戊炔草胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO: 200 mg/mL (780.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9043 mL	19.5213 mL	39.0427 mL
5 mM	0.7809 mL	3.9043 mL	7.8085 mL
10 mM	0.3904 mL	1.9521 mL	3.9043 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： ≥99%

Data Sheet

产品使用指南

Kiessig S, et al. Transcriptional insights into liver toxicity from mixture effects of pesticides and natural toxins: A case study of propyzamide and microcystins. Toxicology. 2026 Dec;527:154580.

Wojtczak A. Differentiation Disorders of Chara vulgaris Spermatids following Treatment with Propyzamide. Cells. 2023 Apr 27;12(9):1268.

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体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

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Other Forms of Rapamycin:

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The molarity calculator equation

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动物实验计算换算器