GLPBio

OD 36 hydrochloride

Catalog No.: GC50517Purity:>99.50%
COASDSData Sheet
OD 36 Hydrochlorid ist ein RIPK2-Inhibitor mit einem IC50 von 5,3 nM.

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OD 36 hydrochloride
Cas No.: 1638644-62-8
1mgIn Stock
$29.00
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5mgIn Stock
$70.00
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10mgIn Stock
$103.00
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25mgIn Stock
$173.00
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50mgIn Stock
$261.00
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Beschreibung (Description)

OD 36 hydrochloride is a potent inhibitor of RIPK2 kinase with an IC50 value of 5.3nM [1]. OD 36 hydrochloride mimics the interaction between the ATP adenine ring and the hinge region of RIPK2 KD, and utilizes the interaction between the cyclic linker group and the hydrophobic posterior pocket as well as the ribose binding region, thereby enhancing the affinity and selectivity for RIPK2[2]. OD 36 hydrochloride has been widely used in mouse peritonitis models to alleviate inflammation[3].

In vitro, OD 36 hydrochloride treatment (0.5μM) for 21 days significantly inhibited the osteogenic and chondrogenic differentiation induced by activin A in ATDC5 cells expressing mutant R206H ALK2 [4]. The 5.3nM OD 36 hydrochloride treatment for 24 hours significantly inhibited the invasion and metastasis of K7M2 cells promoted by macrophages[5].

In vivo, OD 36 hydrochloride treatment via intraperitoneal injection at a single dose of 6.25mg/kg can reduce the cell infiltration in a muramyl dipeptide (MDP)-induced peritonitis mouse model [6].

References:
[1] Shen S, Lu C, Ling T, et al. Current advances on RIPK2 and its inhibitors in pathological processes: a comprehensive review[J]. Frontiers in Molecular Neuroscience, 2025, 18: 1492807.
[2] Pham A T, Ghilardi A F, Sun L. Recent advances in the development of RIPK2 modulators for the treatment of inflammatory diseases[J]. Frontiers in pharmacology, 2023, 14: 1127722.
[3] You J, Wang Y, Chen H, et al. RIPK2: a promising target for cancer treatment[J]. Frontiers in pharmacology, 2023, 14: 1192970.
[4] Sánchez Duffhues G, Williams E, Benderitter P, et al. Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva Derived Endothelial Cells[J]. Journal of Bone and Mineral Research Plus, 2019, 3(11): e10230.
[5] Maloney C, Kallis M P, Edelman M, et al. Gefitinib inhibits invasion and metastasis of osteosarcoma via inhibition of macrophage receptor interacting serine-threonine kinase 2[J]. Molecular cancer therapeutics, 2020, 19(6): 1340-1350.
[6] Tigno-Aranjuez J T, Benderitter P, Rombouts F, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease[J]. Journal of Biological Chemistry, 2014, 289(43): 29651-29664.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

ATDC5 cells

Preparation Method

ATDC5 cells were transduced with the same titer of adenoviral particles in the presence of Polybrene (4mg/ml), encoding for either the ALK2wt‐HA or ALK2R206H‐HA. ATDC5 cells were trypsinized and washed once with PBS. There were 3×105 cells counted per micromass, and resuspended in 10μl of culture medium. Very carefully, 100‐μl drops were deposited in the center of the well in a 24‐wells plate and placed in the incubator for 2 hours. Next 500μl of DMEM‐F12 5% fetal bovine serum (FBS) containing 1× ITS were carefully added to the wells. After 24 hours, the medium was replaced by DMEM‐F12 5% FBS containing 1× ITS, supplemented with activin A (100ng/ml), and DMSO, LDN‐193189, OD 36 hydrochloride, or OD52 (0.5μM). The cells were incubated for 21 days before further analysis, refreshing the medium every 5 days. Finally, the cells were washed and pictures acquired using a microscope with 10× magnification.

Reaction Conditions

0.5μM; 21 days

Applications

OD 36 hydrochloride treatment significantly inhibited the osteogenic and chondrogenic differentiation induced by activin A in ATDC5 cells expressing mutant R206H ALK2.
Animal experiment [2]:

Animal models

C57BL/6 mice

Preparation Method

C57BL/6 mice were housed in an air-conditioned room with a 12h light/dark cycle and received standard laboratory rat chow and tap water. Rats were allowed 7 days to adjust to their new environment. C57BL/6 mice were given vehicle or 6.25mg/kg of Gefitinib or OD 36 hydrochloride intraperitoneal in a 500μl volume. Thirty minutes later, mice were injected with 150μg of MDP intraperitoneal. Four hours later, mice were sacrificed and a peritoneal lavage using 5ml of PBS was performed.

Dosage form

6.25mg/kg for once; i.p.

Applications

OD 36 hydrochloride treatment reduced the cell infiltration in a muramyl dipeptide (MDP)-induced peritonitis mouse model.

References:
[1] Sánchez Duffhues G, Williams E, Benderitter P, et al. Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva Derived Endothelial Cells[J]. Journal of Bone and Mineral Research Plus, 2019, 3(11): e10230.
[2] Tigno-Aranjuez J T, Benderitter P, Rombouts F, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease[J]. Journal of Biological Chemistry, 2014, 289(43): 29651-29664.

Produktdokumente (Product Documents)

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
1638644-62-8
SMILES
ClC1=CC(C2=C3N=C(NCCOCCO4)C=CN3N=C2)=CC4=C1.Cl
Summenformel
C16H15ClN4O2.HCl
Molekulargewicht
367.23
Löslichkeit
DMSO : 33.33 mg/mL (100.76 mM; ultrasonic and warming and heat to 60°C)
Lagerung
Store at 2-8°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

Reviews

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