2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  3. VDAC PERK
  4. NCATS-SM0225

NCATS-SM0225 是一种内质网相关降解 (ERAD) 抑制剂，也是 VDAC1、VDAC2 和 VDAC3 的直接结合剂。NCATS-SM0225 对 ERAD 的 IC50 为 1.02 μM，与人 VDAC1 结合的 Kd 为 3.13 μM。NCATS-SM0225 会破坏细胞钙稳态，增强 VDAC1-IP3R 偶联并激活 PERK。NCATS-SM0225 可选择性杀伤癌细胞，在黑色素瘤异种移植模型中表现出肿瘤生长抑制作用。NCATS-SM0225 可用于包括黑色素瘤在内的多种癌症，以及 ERAD 和钙稳态调控分子机制的研究。

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NCATS-SM0225

NCATS-SM0225 Chemical Structure

CAS No. : 1212623-02-3

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NCATS-SM0225 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2 and VDAC3. NCATS-SM0225 exhibits an IC50of 1.02 μM for ERAD and a Kd of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation[1].

IC50 & Target[1]

VDAC1

3.13 μM (Kd)

VDAC2

 

VDAC3

 

体外研究
(In Vitro)

NCATS-SM0225 (0-12800 nM; 30 min) 可直接结合重组人源 VDAC1，通过 MST[1] 测得其 Kd 为 3.13 μM。
NCATS-SM0225 (2 μM; 1 h) 可与 HeLa 细胞中的 VDAC1、VDAC2 和 VDAC3 全部结合，VDAC 蛋白热稳定性的提升可证明这一点[1]。
NCATS-SM0225 (100-400 nM) 可通过促进其在更低负电位下的电压依赖性关闭来调控 VDAC1 通道功能，其功能学 IC50 为 140 nM[1]。
NCATS-SM0225 (0.625-5 μM; 6 h) 可强效抑制 HeLa 细胞中的 ER 位错，经 NHK-drGFP 报告基因实验检测其 IC50 为 1.02 μM[1]。
NCATS-SM0225 (0.625-5 μM; 6-22 h) 以依赖于 VDAC 的方式升高 HeLa 细胞中线粒体、细胞质和内质网内的钙水平，且该效应会随浓度升高和孵育时间延长而增强[1]。
NCATS-SM0225 (0-10 μM; 40-48 h) 可在部分癌细胞系中选择性诱导凋亡性细胞死亡，同时不损伤正常细胞；其选择性与其破坏钙稳态及降解 ERAD 复合物蛋白的能力相关[1]。
NCATS-SM0225 (1.25-10 μM; 6-24 h) 可在 HeLa 细胞中以剂量依赖、时间依赖且依赖 calcium2+ 的方式选择性诱导 ERAD 复合物蛋白 (HERP1、OS9、FAM8A1) 降解，同时激活 PERK 信号通路[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NCATS-SM0225 相关抗体:

Cell Viability Assay[1]

Cell Line: HeLa, Huh7, A375, U251, U87, PSN1, U2OS, MCF7ca, A253, BT474, MDA-MB-231, SKBR-3, T47D, MDA-MB-453, primary fibroblasts HDFa, GM05294, GM04390, primary melanocytes HEMa, primary hepatocytes
Concentration: 0, 2, 4, 6, 8, 10 μM
Incubation Time: 48 h
Result: Selectively induced cell death in a subset of cancer cell lines (HeLa, Huh7, A375, U251, U87, PSN1, U2OS, MCF7ca, A253, BT474) with significant viability reduction.
Caused minimal to no viability effect on insensitive cancer cell lines (MDA-MB-231, SKBR-3, T47D, MDA-MB-453) and normal cells up to 10 μM.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 1.25, 2.5, 5, 10 μM
Incubation Time: 6 h; 24 h
Result: Reduced HERP1, OS9, and FAM8A1 protein levels in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 6 h
Result: Induced phosphorylation of PERK.
体内研究
(In Vivo)

NCATS-SM0225 (20 mg/kg；腹腔注射；每日一次，持续 14 天) 可显著抑制雄性 BALB/c-nu 小鼠体内 A375 黑色素瘤异种移植瘤的生长，且无可检测到的毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c-nu nude mice (7 weeks old) were subcutaneously injected with A375 human melanoma cells (2 × 106 cells per mouse) which were suspended in a 1:1 mixture with Matrigel into the right flank[1]
Dosage: 20 mg/kg
Administration: intraperitoneal injection; once daily for 14 days
Result: Markedly inhibited tumor growth.
Showed no clinical signs of adverse effects.
Revealed no abnormalities in histological examination of the liver, pancreas, and kidney.
分子量

460.61

Formula

C23H28N2O4S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NCATS-SM0225 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NCATS-SM02251212623-02-3VDACPERKVoltage-dependent anion channel Protein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseERAD inhibitorVDAC1/2/3 direct binderPERK activatorselective anticancer activitycalcium homeostasis disruptorER-phagy activatormelanomagliomabreast cancerliver cancerpancreatic cancerA375 cellsU-251 MG cellsU-87 MG cellsMDA-MB-231 cellsHepG2 cellsHuh7 cellsPSN1 cellsMIAPaCa-2 cellsU-2OS cellsA253 cellsmelanoma xenograft modelInhibitorinhibitorinhibit

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