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TMX-4100 Sale

目录号 : GC63520

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 Chemical Structure

Cas No.:2367619-63-2

规格 价格 库存 购买数量
5 mg
¥2,700.00
现货
10 mg
¥4,320.00
现货
25 mg
¥8,550.00
现货
50 mg
¥13,050.00
现货
100 mg
¥20,250.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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].

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].

[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.

Chemical Properties

Cas No. 2367619-63-2 SDF
分子式 C11H10N4O2S 分子量 262.29
溶解度 储存条件 Store at -20°C
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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
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Research Update

Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216

J Med Chem 2022 Jan 13;65(1):747-756.PMID:34965125DOI:10.1021/acs.jmedchem.1c01832

Immunomodulatory drugs are a class of drugs approved for the treatment of multiple myeloma. These compounds exert their clinical effects by inducing interactions between the CRL4CRBN E3 ubiquitin ligase and a C2H2 zinc finger degron motif, resulting in degradation of degron-containing targets. However, although many cellular proteins feature the degron motif, only a subset of those are degradable via this strategy. Here, we demonstrated that FPFT-2216, a previously reported "molecular glue" compound, degrades PDE6D, in addition to IKZF1, IKZF3, and CK1α. We used FPFT-2216 as a starting point for a focused medicinal chemistry campaign and developed TMX-4100 and TMX-4116, which exhibit greater selectivity for degrading PDE6D and CK1α, respectively. We also showed that the region in PDE6D that interacts with the FPFT-2216 derivatives is not the previously pursued prenyl-binding pocket. Moreover, we found that PDE6D depletion by FPFT-2216 does not impede the growth of KRASG12C-dependent MIA PaCa-2 cells, highlighting the challenges of drugging PDE6D-KRAS. Taken together, the approach we described here represents a general scheme to rapidly develop selective degraders by reprogramming E3 ubiquitin ligase substrate specificity.