PROTAC SAMHD1 Degrader-1

製品番号: HY-182970: Data Sheet 取扱説明書
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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. (Pink: SAMHD1 Target protein ligand (HY-182973); Blue: DCAF1 ligand (HY-182974); Black: linker (HY-W067705)).

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PROTAC SAMHD1 Degrader-1 構造式

容量		在庫状況
MOQ		Minimum order quantity
50 mg		お問い合わせ
100 mg		お問い合わせ
250 mg		お問い合わせ
Other size		お問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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純度とドキュメンテーション
参考文献
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製品説明

体外実験

PROTAC SAMHD1 Degrader-1 (compound NP12) (0.15-10.0 μM; 6-48 h) induces dose- and time-dependent degradation of SAMHD1 in THP-1 cells, with a DC₅₀ of 1.2 μM^[1].
PROTAC SAMHD1 Degrader-1 (10 μM; 24 h pretreatment) increases the sensitivity of wild-type THP-1 cells to Ara-C, reducing the IC₅₀ of Ara-C from 5.4 μM to 1.1 μM, which confirms that it inhibits SAMHD1 activity in cells^[1].
PROTAC SAMHD1 Degrader-1 (1-10 μM; 1 h pretreatment) suppresses the production of LPS (HY-D1056)-induced proinflammatory cytokines (IL-1β, IL-6, TNF-α) in RAW264.7 macrophages in a concentration-dependent manner, and interferes with the transcription, translation and secretion of cytokines^[1].

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

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.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	AUC_0-∞	T_1/2	CL	V_ss	MRT_0-∞	T_max	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 %

体内実験

PROTAC SAMHD1 Degrader-1 (20-80 mg/kg; p.o.; once daily; for 14 consecutive days) induces dose-dependent degradation of SAMHD1 in mouse lung tissue, delays the progression of Bleomycin (HY-108345)-induced pulmonary fibrosis, alleviates lung tissue damage and collagen deposition, and reduces the levels of pro-inflammatory/pro-fibrotic cytokines^[1].

MedChemExpress (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

1080.64

分子式

C₅₄H₆₇ClFN₁₃O₈

SMILES

OCCCCN(N=C1)C(N=C2NC(CC3)CCN3CC(C=C4)=CC(Cl)=C4OC5=CC(NC(COCCOCCOCC(N(CC6)CCN6C7=CC(N[C@@H](C8)CCCN8C9=CC(F)=CC=C9)=NC=N7)=O)=O)=CC=C5)=C1C(N2)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Chen X, et al. Discovery and Evaluation of a PROTAC Degrader Targeting SAMHD1 for the Treatment of Pulmonary Fibrosis. J Med Chem. Published online April 3, 2026. [Content Brief]