TMX-4116

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TMX-4116 

TMX-4116 是酪蛋白激酶 1α (CK1α) 降解剂。TMX-4116 在 MOLT4、Jurkat 和 MM.1S 细胞中显示出对 CK1α 的降解偏好,DC50 小于 200 nM。TMX-4116 可用于多发性骨髓瘤的研究。

TMX-4116

TMX-4116 Chemical Structure

规格 价格 是否有货
5 mg ¥4800 询问价格 & 货期
10 mg ¥8000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma[1].

IC50 & Target[1]

CK1α

 

体外研究
(In Vitro)

TMX-4116 (compound 16; 1 μM; 4 h) shows a high degradation preference for CK1α in MOLT4 cells[1].
TMX-4116 (250 nM, 4 h) induces primary target degradation of CK1α, while no downregulation of PDE6D, IKZF1, and IKZF3 in MOLT4 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 μM
Incubation Time: 4 hours
Result: Showed a high degradation preference for CK1α.

Western Blot Analysis[1]

Cell Line: MOLT4, Jurkat, and MM.1S cells
Concentration: 0 nM, 40 nM, 200 nM, 1 μM
Incubation Time: 4 hours
Result: Showed a high degradation preference for CK1α with the DC50 value less than 200 nM in MOLT4, Jurkat, and MM.1S cells.

分子量

389.43

Formula

C17H19N5O4S

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.

参考文献
  • [1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

TMX-4113

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TMX-4113 

TMX-4113 是磷酸二酯酶 6D (PDE6D) 和酪蛋白激酶 1α (CK1α) 的降解剂。TMX-4113 可用于癌症研究。

TMX-4113

TMX-4113 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

TMX-4113 is a degrader of phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). TMX-4113 can be used for the research of cancer[1].

IC50 & Target[1]

PDE6D

 

CK1α

 

体外研究
(In Vitro)

TMX-4113 (compound 21; 1 μM; 4 h) shows a high degradation preference for PDE6D and CK1α in MOLT4 cells[1].
TMX-4113 (0 nM, 40 nM, 200 nM, 1µM; 4h) induces degradation of PDE6D in MOLT4 cells[1].
TMX-4113 (0 nM, 40 nM, 200 nM, 1µM; 4h) degrades over 50% of CK1α at a dose of 40 nM in MM.1S cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 μM
Incubation Time: 4 h
Result: Showed a high degradation preference for PDE6D and CK1α.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 0 nM, 40 nM, 200 nM, 1µM
Incubation Time: 4 h
Result: Induced degradation of PDE6D.

分子量

308.38

Formula

C12H12N4O2S2

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.

参考文献
  • [1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

TMX-4100

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TMX-4100  纯度: 98.42%

TMX-4100 是一种选择性磷酸二酯酶 6D (PDE6D) 降解剂。TMX-4100 在 MOLT4、Jurkat 和 MM.1S 肿瘤细胞中表现出对 PDE6D 的高降解偏好,DC50 值小于 200 nM。TMX-4100 可用于多发性骨髓瘤的研究。

TMX-4100

TMX-4100 Chemical Structure

CAS No. : 2367619-63-2

规格 价格 是否有货 数量
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
25 mg ¥9500 In-stock
50 mg ¥14500 In-stock
100 mg ¥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

TMX-4100 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma[1].

IC50 & Target[1]

PDE6D

 

体外研究
(In Vitro)

TMX-4100 (compound 3; 1 μM; 4 h) shows a high degradation preference for PDE6D in MOLT4 cells[1].
TMX-4100 has better proteome-wide degradation selectivity in MOLT4 cells, compare to PDE6D degrader FPFT-2216[1].
TMX-4100 does not impede the growth of KRAS-dependent cell lines (MIA PaCa-2, NCI-H358, AGS, PA-TU-8988T cells)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 μM
Incubation Time: 4 hours
Result: Showed a high degradation preference for PDE6D.

Western Blot Analysis[1]

Cell Line: MOLT4, Jurkat, and MM.1S cells
Concentration: 0 nM, 40 nM, 200 nM, 1 μM;
Incubation Time: 4 hours
Result: Showed a high degradation preference for PDE6D with the DC50 value less than 200 nM.

分子量

262.29

Formula

C11H10N4O2S

CAS 号

2367619-63-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (381.26 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8126 mL 19.0629 mL 38.1257 mL
5 mM 0.7625 mL 3.8126 mL 7.6251 mL
10 mM 0.3813 mL 1.9063 mL 3.8126 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.71 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 0.71 mg/mL (2.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.71 mg/mL (2.71 mM); Clear solution

    此方案可获得 ≥ 0.71 mg/mL (2.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务