country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-183717

Copy Link Print Information

M4K3233

M4K3233 is a selective ALK2 PROTAC degrader with a pDC₅₀ of 7.3 and a pIC₅₀ of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma.
(Pink: ALK2 ligand (HY-149591); Blue: Cereblon ligand (HY-14658); Black: linker).

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: C₄₄H₄₈N₆O₇
分子量:772.89

保管条件:

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

M4K3233 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

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

M4K3233 is a selective ALK2 PROTAC degrader with a pDC₅₀ of 7.3 and a pIC₅₀ of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma^[1]. (Pink: ALK2 ligand (HY-149591); Blue: Cereblon ligand (HY-14658); Black: linker).

体外実験

M4K3233 (1 μM; 24 h) is a selective ALK2 degrader in ALK2-overexpressing HEK-293 cells and U87-MG glioblastoma cells, significantly reducing ALK2 levels alongside a small set of off-target proteins including PDE6D, FIZ1, SIK3, and RIPK2, while sparing most other kinases^[1].
M4K3233 (serial dilutions; 4 h) promotes ternary complex formation between ALK2 and CRBN in HEK-293 cells with an apparent pEC₅₀ of 7.42, as measured by a NanoBRET PPI assay^[1].
M4K3233 (0.0002-30 μM; 8 days) inhibits proliferation of patient-derived PDHGG cell lines with GI₅₀ values from 0.3 μM to 5 μM, but this effect appears independent of CRBN-mediated ALK2 degradation^[1].
M4K3233 (0.0002-30 μM; 4 days) reduces viability of U87-MG glioblastoma cells, but this cytotoxic effect is independent of CRBN-mediated ALK2 degradation^[1].

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

Western Blot Analysis^[1]

Cell Line:

ALK2-HiBiT transfected HEK-293 cells
Concentration:

1 μM (M4K3233, 24 h incubation); 20 μM pomalidomide (20 min pretreatment); 20 μM M4K2009 (20 min pretreatment); 1 μM MG132 (20 min pretreatment); 1 μM bafilomycin A1 (20 min pretreatment)
Incubation Time:

24 h (M4K3233 treatment); 20 min (pretreatments)
Result:

Blocked ALK2 degradation when cells were pretreated with either pomalidomide or M4K2009, confirming reliance on both ALK2 and CRBN binding.
Partially recovered ALK2 levels when cells were pretreated with either MG132 or bafilomycin A1, while combined pretreatment with both inhibitors completely blocked ALK2 degradation.

化学情報

分子量 772.89
分子式 C₄₄H₄₈N₆O₇
SMILES

CC1=C(C2=CC=C(N3CCN(CC4CCN(C5=CC=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=C5)CC4)CC3)C=C2)C=NC=C1C8=CC(OC)=C(OC)C(OC)=C8
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]. Webb DT, et al. Targeting Activin Receptor-like Kinase 2 Using Heterobifunctional Protein Degraders. J Med Chem. 2026;69(9):11524-11546. [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

お問い合わせ在庫あり

Other size

お問い合わせ