2. PROTAC Anti-infection Immunology/Inflammation
  3. PROTACs HIV Interleukin Related
  4. PROTAC SAMHD1 Degrader-1

PROTAC SAMHD1 Degrader-1 是一种口服有效的靶向 SAMHD1 PROTAC 降解剂，对 SAMHD1 的 dNTP 水解酶的 IC50 为 6.3 μM。PROTAC SAMHD1 Degrader-1 可在细胞内与 SAMHD1 结合并介导其降解，且脱靶效应较低。PROTAC SAMHD1 Degrader-1 可抑制促炎细胞因子生成，干扰炎症反应级联放大过程。PROTAC SAMHD1 Degrader-1 可延缓肺纤维化进展，并发挥肺组织保护作用。PROTAC SAMHD1 Degrader-1 可用于肺纤维化相关研究。
(粉色: Ligands for Target Protein for PROTAC 和 HIV 配体 (HY-182973)；蓝色: Ligands for E3 Ligase 配体 (HY-182974)；黑色: 连接子 (HY-W067705))。

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PROTAC SAMHD1 Degrader-1

PROTAC SAMHD1 Degrader-1 Chemical Structure

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PROTAC SAMHD1 Degrader-1 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC SAMHD1 Degrader-1 is an orally active targeted SAMHD1 PROTAC degrader, with an IC50 of 6.3 μM against the dNTP hydrolase activity of SAMHD1. PROTAC SAMHD1 Degrader-1 binds to SAMHD1 inside cells and mediates its degradation, with low off-target effects. PROTAC SAMHD1 Degrader-1 inhibits the production of pro-inflammatory cytokines and interferes with the cascade amplification process of inflammatory responses. PROTAC SAMHD1 Degrader-1 delays the progression of pulmonary fibrosis and exerts protective effects on lung tissues. PROTAC SAMHD1 Degrader-1 can be used in pulmonary fibrosis-related research[1]. (Pink: Ligands for Target Protein for PROTAC and HIV ligand (HY-182973); Blue: Ligands for E3 Ligase ligand (HY-182974); Black: linker (HY-W067705)).

体外研究
(In Vitro)

PROTAC SAMHD1 Degrader-1 (compound NP12) (0.15-10.0 μM; 6-48 h) 可在 THP-1 细胞中诱导 SAMHD1 呈剂量和时间依赖性降解，DC50 为 1.2 μM[1]。
PROTAC SAMHD1 Degrader-1 (10 μM; 24 h pretreatment) 可提高野生型 THP-1 细胞对 Ara-C 的敏感性，将 Ara-C 的 IC50 从 5.4 μM 降至 1.1 μM，证实其可在细胞内抑制 SAMHD1 的活性[1]。
PROTAC SAMHD1 Degrader-1 (1-10 μM; 1 h pretreatment) 可以浓度依赖方式抑制 RAW264.7 巨噬细胞中 LPS (HY-D1056) 诱导的促炎细胞因子 (IL-1β、IL-6、TNF-α) 产生，干扰细胞因子的转录、翻译与分泌[1]。

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

PROTAC SAMHD1 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-1 human acute monocytic leukemia cells
Concentration: 0.15, 0.3, 0.6, 1.2, 2.5, 5.1, 10.0 μM
Incubation Time: 6 h, 24 h, 48 h
Result: Induced 47.9%, 74.4%, and 91.8% SAMHD1 degradation at 1 μM, 2.5 μM, and 5 μM for 48 h, respectively.
Showed dose-dependent degradation across 0.15-10.0 μM for 48 h, with a DC50 of 1.2 μM.
Achieved 66% degradation at 24 h and maximum 89% degradation at 48 h with 5 μM treatment.
Maintained suppressed SAMHD1 levels for at least 24 h post-withdrawal of 5 μM treatment, with levels returning to near initial levels by 48 h post-withdrawal.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t AUC0-∞ T1/2 CL Vss MRT0-∞ Tmax Bioavailability
Rat[1] 2 mg/kg i.v. 1226.5 ng/mL 2391.4 ng·h/mL 2941.1 ng·h/mL 3.9 h 837.5 mL/h/kg 2.9 L/kg 3.5 h / /
Rat[1] 30 mg/kg p.o. 437.3 ng/mL 5308.4 ng·h/mL 7165.5 ng·h/mL 3.5 h / / / 6.0 h 16.2 %
体内研究
(In Vivo)

PROTAC SAMHD1 Degrader-1 (20-80 mg/kg；灌胃；每日一次；连续 14 天) 可诱导小鼠肺组织中 SAMHD1 呈剂量依赖性降解，延缓Bleomycin (HY-108345)诱导的肺纤维化进展，减轻肺组织损伤与胶原沉积，并降低促炎/促纤维化细胞因子水平[1]。

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

Animal Model: C57BL/6 (male, 6-8 weeks old, 18-22 g, intratracheal bleomycin-induced pulmonary fibrosis)[1]
Dosage: 20 mg/kg; 40 mg/kg; 80 mg/kg
Administration: i.g.; daily; 14 days
Result: Showed gradual body weight recovery from day 9 onward.
Reduced bleomycin-induced lung tissue damage, including alleviated alveolar atrophy/collapse, bronchial wall thickening, and inflammatory cell infiltration.
Decreased collagen fiber deposition in a dose-dependent manner.
Significantly downregulated lung tissue expression of α-smooth muscle actin and fibronectin in a dose-dependent manner.
Reduced serum and bronchoalveolar lavage fluid levels of proinflammatory and profibrotic cytokines (IL-1β, IL-6, TGF-β1), with the 80 mg/kg dose showing the most pronounced effects.
Reduced lung tissue SAMHD1 protein levels to 80.7% (20 mg/kg), 58.3% (40 mg/kg), and 21.9% (80 mg/kg) of the control group, demonstrating dose-dependent degradation.
分子量

1079.66

Formula

C55H68ClFN12O8
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 SAMHD1 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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

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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 SAMHD1 Degrader-1PROTACsHIVInterleukin RelatedHuman immunodeficiency virusILRAW264.7 macrophagesIL-1βSAMHD1TNF-αpulmonary fibrosisTHP-1 cellsDCAF1bleomycin-induced mouse modelubiquitin-dependent CRL-proteasome pathwayIL-6Inhibitorinhibitorinhibit

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