2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. SD-965

SD-965 是一种选择性的 STAT3 PROTAC 降解剂，其 DC50 为 0.14 μM。SD-965 能促进 STAT3 的泛素化和降解。SD-965 可诱导 STAT3 蛋白快速、完全且持久地耗竭。SD-965 可在白血病和淋巴瘤的小鼠异种移植模型中诱导肿瘤消退。
(粉色: STAT3 靶蛋白配体；蓝色: Cereblon 配体 (HY-W1009348)；黑色: 连接子 (HY-W017522))。

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SD-965

SD-965 Chemical Structure

CAS No. : 3054394-56-5

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SD-965 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SD-965 is a selective STAT3 PROTAC degrader with a DC50 of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma[1]. (Pink: STAT3 Target protein ligand; Blue: Cereblon ligand (HY-W1009348); Black: linker (HY-W017522)).

IC50 & Target[1]

STAT3

0.14 μM (DC50)

体外研究
(In Vitro)

SD-965 (up to 5 μM; 24 h) 在 STAT3 HiBiT 分析中可强效降解 STAT3，其 DC50 为 0.14 μM，孵育 24 h 后最大降解率达 85%[1]。
SD-965 可强效抑制 MOLM-16 白血病细胞 (IC50 = 1.3 nM) 和 SU-DHL-1 淋巴瘤细胞的生长 (IC50 = 260 nM)[1]。
SD-965 (3.2-2000 nM; 14 h) 可选择性降解 STAT3，在外周血单个核细胞中孵育 14 小时后最大降解率超过 90%，在浓度高达 2 μM 时对其他 STAT 家族蛋白无显著影响[1]。
SD-965 在小鼠、大鼠、犬、猴体系中表现出优异的微粒体稳定性与血浆稳定性，在所有受试基质中的半衰期均 >120 min[1]。

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

SD-965 相关抗体:

Western Blot Analysis[1]

Cell Line: SU-DHL-1 human anaplastic large cell lymphoma cells
Concentration: 3.2-2000 nM
Incubation Time: 14 h
Result: Degraded STAT3 with a DC50 of 80 nM and a Dₘₐₓ of >90%.
Showed no obvious effect on STAT1 or STAT6, modestly reduced STAT2 and STAT5 at 2 μM, and increased STAT4 levels in a dose-dependent manner.
体内研究
(In Vivo)

SD-965 (25-50 mg/kg; 静脉注射; 每周一次; 持续 3-4 周) 在 SU-DHL-1 淋巴瘤异种移植瘤小鼠模型中能有效抑制肿瘤生长[1]。

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

Animal Model: SU-DHL-1 lymphoma xenograft mouse model[1]
Dosage: 25-50 mg/kg
Administration: i.v.; once weekly; for 3-4 consecutive weeks
Result: Induced a maximum tumor regression by 58% at 25 mg/kg.
Reduced the tumor volume by 52% on day 5 after the first dose and by 96% on day 16, with 60% of mice without palpable tumors (50 mg/kg).
分子量

1213.21

Formula

C56H65N10O17PS
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

SD-965 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

SD-9653054394-56-5SD965SD 965PROTACsSTATleukemiaMOLM-16STAT3proteasomecereblonNEDD8-activating enzymemouse xenograft modelslymphomahuman PBMCsSU-DHL-1Inhibitorinhibitorinhibit

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