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製品番号: HY-159570

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XD2-149

XD2-149 is a ZFP91 PROTAC degrader with DC₅₀ values of 0.08 μM and 0.06 μM, respectively. ZFP91 is a bifunctional nuclear protein with both transcription factor and E3 ubiquitin ligase activities, and is classified as an oncogenic non-canonical NF-κB pathway regulator in tumor and immune regulation. XD2-149 induces proteasome-dependent degradation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 inhibits the STAT3 signaling pathway in pancreatic cancer cells and induces NQO1-dependent cell death independent of ZFP91 degradation. XD2-149 can be used for the research of pancreatic cancer.
(Pink: STAT3 ligand (HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).

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。

CAS 番号: 2710221-08-0
分子式: C₃₈H₃₉N₅O₈
分子量:693.74

保管条件:

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

Data Sheet (270 KB)

XD2-149 構造式

CAS 番号: 2710221-08-0

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
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

XD2-149 is a ZFP91 PROTAC degrader with DC₅₀ values of 0.08 μM and 0.06 μM, respectively. ZFP91 is a bifunctional nuclear protein with both transcription factor and E3 ubiquitin ligase activities, and is classified as an oncogenic non-canonical NF-κB pathway regulator in tumor and immune regulation. XD2-149 induces proteasome-dependent degradation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 inhibits the STAT3 signaling pathway in pancreatic cancer cells and induces NQO1-dependent cell death independent of ZFP91 degradation. XD2-149 can be used for the research of pancreatic cancer^[1]. (Pink: STAT3 ligand (HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).

IC₅₀ & Target^[1]

ZFP91

0.06 μM (DC₅₀)

STAT3

PROTACs アイソフォーム固有の製品をすべて表示 :

STAT アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.8 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1.2 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	2.1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
HEK293	IC₅₀	8.7 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33506674]
MIA PaCa-2	IC₅₀	1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]

体外実験

XD2-149 (72 h) potently inhibits the proliferation of MIA PaCa-2 and BxPC-3 pancreatic cancer cells with an IC₅₀ of 0.9 μM for both, and its cytotoxicity is partially dependent on the expression of ZFP91^[1].
XD2-149 (0-0.5 μM; 7-10 days) inhibits colony formation of BxPC-3 pancreatic cancer cells^[1].
XD2-149 (24 h) potently inhibits STAT3-mediated transcription activated by IL-6 in HEK-293 cells, with an IC₅₀ of 0.9 μM^[1].
XD2-149 potentiates Cycloheximide (HY-12320)-mediated inhibition of STAT3 protein synthesis, and induces NQO1 downregulation in BxPC-3 pancreatic cancer cells in a de novo protein synthesis-dependent manner^[1].
XD2-149 (16 h) downregulates 84 proteins (including STAT3 and ZFP91) in BxPC-3 pancreatic cancer cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

BxPC-3 cells
Concentration:

0, 0.06, 0.13, 0.25, 0.5 μM
Incubation Time:

7-10 days
Result:

Inhibited colony formation.

化学情報

CAS 番号 2710221-08-0
分子量 693.74
分子式 C₃₈H₃₉N₅O₈
SMILES

O=C(C1=CC2=C(C(C3=C(C2=O)C=CC=C3)=O)O1)NCCN4CCC(CCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)CC4
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 (270 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]. Hanafi M, et al. Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91. Journal of medicinal chemistry. 2021 Feb 11;64(3):1626-1648. [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.

Bioz

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
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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数量:
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XD2-149

PROTACs アイソフォーム固有の製品をすべて表示

STAT アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示