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Cat. No.: HY-148382

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RI-962

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Based on 1 Customer Validation

RI-962 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor. RI-962 inhibits RIPK1 with an IC₅₀ value of 35.0 nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases.

For research use only. We do not sell to patients.

Purity: 99.50%
CAS No.: 2763831-53-2
Formula: C₂₈H₂₈N₆O₂
Molecular Weight:480.56

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RI-962 Chemical Structure

CAS No.: 2763831-53-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 35.0 nM (RIPK1); EC50: 10.0 nM (HT29 cells), 4.2 nM (L929 cells), 11.4 nM (J774A.1 cells), 17.8 nM (U937 cells)^[1].

All RIP kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC₅₀	10 nM Compound: RI-962	Protection against TSZ-induced necroptosis in human HT-29 cells preincubated with compound followed by TNA-alpha,Smac mimetic and Z-VAD-FMK addition and measured after 24 hrs by CCK-8 assay Protection against TSZ-induced necroptosis in human HT-29 cells preincubated with compound followed by TNA-alpha,Smac mimetic and Z-VAD-FMK addition and measured after 24 hrs by CCK-8 assay	[PMID: 38159286]

In Vitro

RI-962 has potent inhibitory activity for RIPK1 with an IC₅₀ value of 35.0 nM^[1].
RI-962 has protective effect for necroptotic death with EC₅₀ values of 10.0 nM, 4.2 nM, 11.4 nM, and 17.8 nM for HT29, L929, J774A.1, and U937 cells, respectively^[1].
RI-962 (0-100 μM; 24 h) protectes cells from TSZ-induced necroptosis by inhibiting the kinase activity of RIPK1^[1].

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

Cell Viability Assay^[1]

Cell Line:

HT29, L929, J774A.1, and U937 cells
Concentration:

0-100 μM
Incubation Time:

24 h
Result:

Exerted a dose-dependent protective effect against necroptotic death.

Western Blot Analysis^[1]

Cell Line:

HT29 cells
Concentration:

0-400 nM
Incubation Time:
Result:

Markedly inhibited the phosphorylation of RIPK1 and its downstream signaling proteins RIPK3 and MLKL in a dose-dependent manner.

In Vivo

RI-962 (i.p.; 40 mg/kg; once a day for 10 day) ameliorates TNFα-induced SIRS and reduces inflammation in acute DSS (HY-116282C)-induced colitis^[1].
Pharmacokinetic Parameters of RI-962 in rats (i.v., i.p., p.o.; 5, 20 mg/kg) ^[1].

RI-962	i.v.	p.o.	i.p.
Dose (mg/kg)	5	20	20
T_1/2 (h)	2.1 ± 0.2	1.3 ± 0.2	8.5 ± 1.6
T_max (h)	0.1 ± 0.0	0.8 ± 1.0	0.5 ± 0.0
C_max (ng/mL)	12170.4 ± 1198.5	674.2 ± 424.7	3603.3 ± 693.3
AUC_0-t(ng*h/mL)	4526.1 ± 546.0	1594.9 ± 891.8	6459.7 ± 1131.6
AUC_0-∞ (ng*h/mL)	4538.1 ± 546.3	1604.5 ± 896.1	6609.3 ± 1121.4
V_ss (L/kg)	0.4 ± 0.1	-	-
MRT_0-∞ (h)	0.4 ± 0.0	1.8 ± 0.2	2.8 ± 0.1
CL (mL/min/kg)	18.5 ± 2.1	-	-
F (%)	-	8.8 ± 5.0	35.7 ± 6.3

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

Animal Model:

C57BL/6 female mice^[1]
Dosage:

40 mg/kg
Administration:

Intraperitoneal for 15 min; once a day for 10 day
Result:

Ameliorated TNFα-induced SIRS by inhibiting RIPK1 activity.
Suppressed the RIPK1 signaling in the mouse model of DSS-induced colitis.

Animal Model:

Sprague-Dawley (SD) rats^[1]
Dosage:

5, 20 mg/kg
Administration:

intravenous (i.v.) (5 mg/kg), intraperitoneal (i.p.) (20 mg/kg) and oral (p.o.) (20 mg/kg)
Result:

Had good metabolic stability in rats.

Chemical Information

CAS No. 2763831-53-2
Appearance Solid
Molecular Weight 480.56
Formula C₂₈H₂₈N₆O₂
Color Off-white to light yellow
SMILES

O=C(C1=CN(C)C2=C1C=C(C3=CC4=NC(NC(C(C)C)=O)=NN4C=C3)C=C2)NC(C)C5=CC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (208.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0809 mL

10.4045 mL

20.8091 mL

5 mM

0.4162 mL

2.0809 mL

4.1618 mL

10 mM

0.2081 mL

1.0405 mL

2.0809 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[1]. Yueshan Li, et al. Generative deep learning enables the discovery of a potent and selective RIPK1 inhibitor. Nat Commun. 2022 Nov 12;13(1):6891. [Content Brief]

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.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0809 mL	10.4045 mL	20.8091 mL	52.0226 mL
	5 mM	0.4162 mL	2.0809 mL	4.1618 mL	10.4045 mL
	10 mM	0.2081 mL	1.0405 mL	2.0809 mL	5.2023 mL
	15 mM	0.1387 mL	0.6936 mL	1.3873 mL	3.4682 mL
	20 mM	0.1040 mL	0.5202 mL	1.0405 mL	2.6011 mL
	25 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0809 mL
	30 mM	0.0694 mL	0.3468 mL	0.6936 mL	1.7341 mL
	40 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3006 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0405 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8670 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL
	100 mM	0.0208 mL	0.1040 mL	0.2081 mL	0.5202 mL

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

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RI-962

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Protein-protein Interaction Inhibitor Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All RIP kinase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RI-962

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Protein-protein Interaction Inhibitor Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All RIP kinase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RI-962 Related Classifications

Cat. No.: HY-148382