2. PROTAC Metabolic Enzyme/Protease Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Epigenetics Apoptosis
  3. PROTACs E1/E2/E3 Enzyme DNA/RNA Synthesis JAK STAT Apoptosis
  4. PROTAC SKP2 Degrader-1

PROTAC SKP2 Degrader-1 是一种靶向 SKP2 的 PROTAC 降解剂，Kd 为 6.28 μM。PROTAC SKP2 Degrader-1 可通过泛素-蛋白酶体系统诱导 SKP2 的靶向降解。PROTAC SKP2 Degrader-1 可稳定 SOCS1 的表达，并通过 JAK/STAT 通路调节免疫蛋白酶体的表达，从而抑制肿瘤细胞增殖。PROTAC SKP2 Degrader-1 可用于癌症相关研究。
(粉色: Skp2 配体 (HY-N0256)；蓝色: VHL 配体 (HY-125845)；黑色: 连接子 (HY-140189))。

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PROTAC SKP2 Degrader-1

PROTAC SKP2 Degrader-1 Chemical Structure

CAS No. : 3120650-15-6

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PROTAC SKP2 Degrader-1 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 DNA/RNA Synthesis 亚型特异性产品:

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research[1]. (Pink: Skp2 ligand (HY-N0256); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

IC50 & Target[1]

Skp2

 

STAT1

 

体外研究
(In Vitro)

PROTAC SKP2 Degrader-1 (compound HD15) (48 h) 可抑制 Jurkat 细胞增殖，其 IC50 为 0.98 μM[1]。
PROTAC SKP2 Degrader-1 (0.0625-1 μM; 48 h) 可在 Jurkat 细胞中诱导 SKP2 发生蛋白酶体依赖性降解，其 DC50 为 0.29 μM[1]。
PROTAC SKP2 Degrader-1 (0.0625-1 μM; 48 h) 可在 Jurkat 细胞中调控 SOCS1/JAK/STAT1/免疫蛋白酶体轴，以浓度依赖的方式上调 SOCS1、抑制 p-STAT1 并下调免疫蛋白酶体亚基 PSMB8、PSMB9 和 PSMB10[1]。
PROTAC SKP2 Degrader-1 (0-6 μM; 48 h) 可呈剂量依赖性地抑制 Jurkat 和 Hut78 细胞中的 DNA 合成与增殖[1]。
PROTAC SKP2 Degrader-1 (0.1875-6 μM; 48 h) 可剂量依赖性地诱导 Jurkat 细胞发生细胞凋亡[1]。

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

PROTAC SKP2 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.0625, 0.125, 0.25, 0.5 and 1 μM
Incubation Time: 48 h
Result: Induced concentration-dependent degradation of SKP2 protein in Jurkat cells, with a DC50 of 0.29 μM.
Blocked SKP2 degradation when cotreated with MG132, confirming proteasome-dependent activity.

Apoptosis Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.1875, 0.75, 1.5, 3 and 6 μM
Incubation Time: 48 h
Result: Induced apoptosis in Jurkat cells in a dose-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 MRT0-inf CL AUC0-t AUC0-inf Tmax Cmax CL/F
Mice[1] 10 mg/kg i.v. 1.81 h 0.92 h 48.8 mL/min/kg 3387 ng·h/mL 3441 ng·h/mL / / /
Mice[1] 40 mg/kg i.p. 3.71 h / / 26714 ng·h/mL 26876 ng·h/mL 2.0 h 4497 ng/mL 25 mL/min/kg
体内研究
(In Vivo)

PROTAC SKP2 Degrader-1 (10-40 mg/kg; i.p.; daily; 14 days) 可剂量依赖性地抑制雌性 NCG 小鼠皮下 Jurkat 细胞异种移植瘤的生长[1]。

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

Animal Model: NCG mice (female, 6-7 weeks old, 20-25 g, subcutaneous xenograft via Jurkat cell inoculation)[1]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 14 days
Result: Achieved a 66% tumor growth inhibition (TGI) rate at 40 mg/kg.
Achieved a TGI exceeding 50% at 20 mg/kg.
Reduced tumor volume and weight significantly across all doses compared to vehicle control.
Suppressed SKP2, phosphorylated STAT1, and immunoproteasome subunits PSMB8, PSMB9, and PSMB10 in a dose-dependent manner in tumor tissue.
Upregulated SOCS1 expression in tumor tissue.
Induced dose-dependent tumor cell apoptosis and necrosis.
Reduced microvascular density and proliferation in a dose-dependent manner.
Caused no significant changes in body weight, liver function biomarkers, or kidney function biomarkers across all doses.
Showed no pathological alterations in heart, liver, spleen, lung, or kidney tissues.
分子量

1074.46

Formula

C60H91N5O10S
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

PROTAC SKP2 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PROTAC SKP2 Degrader-13120650-15-6PROTACsE1/E2/E3 EnzymeDNA/RNA SynthesisJAKSTATApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseJanus kinaseJAK/STAT pathwaySKP2T lymphoblastic leukemia cellsHut78 T-ALL cellsJurkat T-ALL cellsInhibitorinhibitorinhibit

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