PROTAC STING Degrader-1

Name: PROTAC STING Degrader-1
Brand: MedChemExpress
SKU: HY-150608
Rating: 4.5 (1 reviews)

製品番号: HY-150608 純度: 98.26%: Data Sheet SDS COA 取扱説明書
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PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC₅₀ of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs).
(Pink: STING ligand (HY-138682); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W015883)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

PROTAC STING Degrader-1 構造式

CAS 番号 : 2762552-74-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 623	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 623	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$135	在庫あり	Estimated Time of Arrival: December 31
5 mg	$405	在庫あり	Estimated Time of Arrival: December 31
10 mg	$645	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1290	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1933	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2899	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* 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.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

顧客検証

•Patent. US20260007648A1.

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC₅₀ of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs)^[1]^[2]^[3]. (Pink: STING ligand (HY-138682); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W015883)).

体外実験

PROTAC STING Degrader-1 (Compound SP23) (2.5-20 μM) downregulates the downstream signals of STING pathway (IFN-β, IL-6, and CXCL10) triggered by cGAMP in THP-1 cells^[1].
PROTAC STING Degrader-1 (1.25-30 μM, 24 h) does not degrade other inflammation-related proteins (JAK2, STAT3, PI₃K, AKT, and TLR4) in THP-1 cells^[1].
PROTAC STING Degrader-1 (0-40 μM, 2-72 h) degrades STING dose- and time-dependently in THP-1 cells^[1].
PROTAC STING Degrader-1 (1.1-30 μM) shows no cytotoxicity in LO2, HEK293A, and C17.2 at doses below 10 μM, but displays a slight cytotoxicity at 30 μM in HEK293A and C17.2 cells^[1].
PROTAC STING Degrader-1 (Compound SP23) reduces the production of proinflammatory cytokines and transcription of ISGs in the colon tissues of mice^[3].
PROTAC STING Degrader-1 exhibits a dose-dependent degradation efficacy of STING in NCM460 cells^[3].

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

Western Blot Analysis^[1]

Cell Line:	THP-1 cells
Concentration:	0, 0.3, 0.625, 1.25, 2.5, 5, 10, 20, 30, 40 μM
Incubation Time:	2, 4, 8, 12, 24, 48, 72 h
Result:	Exhibited the highest degradation efficiency with a DC₅₀ of 3.2 μM. Degradation occurred at 4 h and reached maximum degradation at 48 h.

Parmacokinetics

Species	Dose	Route	AUC	MRT	T_1/2	T_max	Clearance (CL)	V_z	Plasma Concentration	Bioavailability
Rat	2 mg/kg	i.v.	257 ng·h/mL	1.74 h	3.86 h	0.083 h	6.80 L/h/kg	38.01 L/kg	318.2 ng/mL	/
Rat	20 mg/kg	p.o.	52.21 ng·h/mL	7.60 h	7.36 h	3.71 h	429.44 L/h/kg	4480.43 L/kg	8.37 ng/mL	2.15 %

体内実験

PROTAC STING Degrader-1 (Compound SP23) (30-60 mg/kg, i.p. 1 h prior to Cisplatin (HY-17394) injection, same time each day for 4 d) significantly alleviates the ischemic symptoms and the kidney weights reduces dramatically and dose-dependently in Cisplatin-induced acute kidney injury C57BL/6J mouse model^[1].
PROTAC STING Degrader-1 (Compound SP23) (10-30 mg/kg, i.p., 7 consecutive days) ameliorates the severity of DSS-induced colitis in C57BL/6J mice^[3].

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

Animal Model:	Cisplatin-induced acute kidney injury C57BL/6J mouse model^[1]
Dosage:	30 and 60 mg/kg
Administration:	Intraperitoneal injection (i.p.) 1 h prior to Cisplatin injection, same time each day for 4 d
Result:	Resulted in survival rates of 89% (30 mg/kg) and 100% (60 mg/kg). Decreased body weights of mice. Reduced the levels of blood urea nitrogen and creatinine. Improved the renal blood flow and reduced kidney swelling. Significantly alleviated the kidney damages.

Animal Model:	DSS-induced colitis in 8-weeks C57BL/6J mice^[3]
Dosage:	10 and 30 mg/kg
Administration:	Intraperitoneal injection (i.p.) for 7 consecutive days
Result:	Reduced body weight and intestinal mucosal destruction. Ameliorated the colon shortening. Showed a lower disease activity index in mice. Led to a significant increase in total immune cells (CD45⁺). Decreased the macrophage M1 polarization and downregulated the mRNA levels of M1 macrophage marker genes (iNOS and CD86). Increased the tight junction proteins. Downregulated the NLRP3 and cleaved-Capase 1 induced by DSS in mice. Abrogated the mRNA level of NLRP3 and IL-18.

分子量

699.67

分子式

C₃₄H₃₃N₇O₁₀

CAS 番号

2762552-74-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)/C=C/C(NC4=CC=C(NC(C5=CC=C([N+]([O-])=O)O5)=O)C=C4)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (142.92 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4292 mL	7.1462 mL	14.2925 mL
5 mM	0.2858 mL	1.4292 mL	2.8585 mL
10 mM	0.1429 mL	0.7146 mL	1.4292 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 98.26%

Select Batch:

データシート (277 KB) SDS (252 KB)

COA (245 KB) HNMR (204 KB) RP-HPLC (207 KB) LCMS (104 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Liu J, et al. Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy. J Med Chem. 2022 May 12;65(9):6593-6611. [Content Brief]

[2]. Rongxiang Ma, et al., Discovery of novel rigid STING PROTAC degraders as potential therapeutics for acute kidney injury, European Journal of Medicinal Chemistry, Volume 290, 2025, 117539, ISSN 0223-5234. [Content Brief]

[3]. Shuai Xu, et al., PROTAC based STING degrader attenuates acute colitis by inhibiting macrophage M1 polarization and intestinal epithelial cells pyroptosis mediated by STING-NLRP3 axis, International Immunopharmacology, Volume 141, 2024, 112990, ISSN 1567-5769. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4292 mL	7.1462 mL	14.2925 mL	35.7311 mL
	5 mM	0.2858 mL	1.4292 mL	2.8585 mL	7.1462 mL
	10 mM	0.1429 mL	0.7146 mL	1.4292 mL	3.5731 mL
	15 mM	0.0953 mL	0.4764 mL	0.9528 mL	2.3821 mL
	20 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7866 mL
	25 mM	0.0572 mL	0.2858 mL	0.5717 mL	1.4292 mL
	30 mM	0.0476 mL	0.2382 mL	0.4764 mL	1.1910 mL
	40 mM	0.0357 mL	0.1787 mL	0.3573 mL	0.8933 mL
	50 mM	0.0286 mL	0.1429 mL	0.2858 mL	0.7146 mL
	60 mM	0.0238 mL	0.1191 mL	0.2382 mL	0.5955 mL
	80 mM	0.0179 mL	0.0893 mL	0.1787 mL	0.4466 mL
	100 mM	0.0143 mL	0.0715 mL	0.1429 mL	0.3573 mL