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製品番号: HY-170900

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SJ44236

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.
(Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).

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。

分子式: C₄₀H₄₅ClN₈O₃S
分子量:753.36

保管条件:

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

Data Sheet (271 KB)

SJ44236 構造式

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma^[1]. (Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).

IC₅₀ & Target^[1]

BRD4

127 pM (DC₅₀)

BRD2

BRD3

Cereblon

PROTACs アイソフォーム固有の製品をすべて表示 :

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

体外実験

SJ44236 (1×10^-10 to 1×10² μM; 24 h) potently degrades BRD4 in HiBiT-BRD4 HEK293 LgBiT stable cells with a Dmax₅₀ of 0.19 nM, achieving 96.9% maximal degradation sustained for over 20 h with no impact on cell viability^[1].
SJ44236 (0.001-100 nM; 4 h) degrades endogenous BRD4 in MV4-11 cells with a DC₅₀ of 0.127 nM after 4 h of treatment, consistent with its potency in engineered HEK293 cells^[1].
SJ44236 (72 h) potently inhibits the proliferation of MV4-11 cells with an IC₅₀ of 0.12 nM and HD-MB03 cells with an IC₅₀ of 0.92 nM after 72 h of treatment^[1].
SJ44236 (100 nM; 4 h) induces over 90% degradation of BRD2, BRD3, and BRD4 in MV4-11 cells after 4 h of treatment at 100 nM, alongside expected downstream regulation of c-Myc (down) and p53 (up)^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	Bioavailability	AUC_last	CL	T_1/2 (Elimination)	AUC	V_d
Mice^[1]	3 mg/kg	i.v.	/	/	/	/	8.85 mL/min/kg	3.4 h	5541 ng·h/mL	0.85 L/kg
Mice^[1]	10 mg/kg	p.o.	2436 ng/mL	0.5 h	45 %	8060 ng·h/mL	/	/	/	/

体内実験

SJ44236 (3-10 mg/kg; i.v., p.o.; single dose) exhibits favorable in vivo pharmacokinetic properties in female CD1 mice, including 45% oral bioavailability, low clearance, and rapid oral absorption^[1].

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

化学情報

分子量 753.36
分子式 C₄₀H₄₅ClN₈O₃S
SMILES

O=C(C[C@@H]1N=C(C2=C(N3C1=NN=C3C)SC(C)=C2C)C4=CC=C(Cl)C=C4)N5CCC(CC5)CN6CCN(C7=CC=C(C=C7)C8C(NC(CC8)=O)=O)CC6
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

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (271 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Actis M, et al. Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs. J Med Chem. 2025;68(3):3591-3611. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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SJ44236

PROTACs アイソフォーム固有の製品をすべて表示

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

SJ44236 関連分類

HY-170900 関連分類