Art. -Nr.: HY-128348

PK68

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PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC₅₀ of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis.

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Reinheit: 99.92%
CAS. Nr.: 2173556-69-7
Formel: C₂₂H₂₄N₄O₃S
Molecular Weight:424.52

Speicherung:

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

PK68 Chemical Structure

CAS. Nr.: 2173556-69-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RIPK1

90 nM (IC₅₀)

RIPK1

23 nM (EC₅₀)

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC₅₀	23 nM Compound: 6; PK68	Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in human HT-29 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition ans measured after 24 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34906762]
L929	EC₅₀	13 nM Compound: 6; PK68	Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in mouse L929 cells assessed as TNFalpha/Z-VAD (TSZ) induced necroptosis by measuring cell viability preincubated for 1 hr followed by TSZ addition and measured after 24 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34906762]

In Vitro

PK68 has highly potent inhibition of TNF-induced necroptosis with EC₅₀ values of 23 nM and 13 nM in human and mouse cells, respectively^[1].
PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC₅₀ value of 90 nM^[1].
PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation^[1].

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

Cell Viability Assay^[1]

Cell Line:

Bone marrow-derived macrophages, NIH3T3-RIPK3 cells
Concentration:

100 nM
Incubation Time:

1 h
Result:

PK68 block cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli.
PK68 inhibit TNF-induced necroptosis but not RIPK3 dimerization-induced cell death in NIH3T3-RIPK3 cells.

Western Blot Analysis^[1]

Cell Line:

HT-29 cells
Concentration:

100 nM
Incubation Time:

1 h
Result:

Completely abolished phosphorylation of RIPK1, RIPK3, and MLKL.

Immunofluorescence^[1]

Cell Line:

HT-29 cells
Concentration:

100 nM
Incubation Time:

1 h
Result:

Prevented generation of RIPK3 puncta.

In Vivo

PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice^[1].
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome^[1].
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis^[1].

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

Animal Model:

C57BL/6 mice^[1]
Dosage:

5 mg/kg, 25 mg/kg
Administration:

5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days
Result:

Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg.

Animal Model:

C57BL/6 mice^[1]
Dosage:

2 mg/kg, 10 mg/kg
Administration:

2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days

Result:

	PO (Gavage)	IV (Bolus)
T_max (hr)	0.5
C_max (ng/mL)	2423
AUC_0-24 (ng/mL•hr)	4821	1588
AUCINF (ng/mL•hr)	4897	1590
t_1/2 (hr)	1.3	1.0
MRT (hr)	1.8	0.8
CL (mL/hr/kg)		1258
CL (mL/min/kg)		21
Vss (mL/kg)		1009
Vss (L/kg)		1.0
F(%)	61

Animal Model:

C57BL/6 mice^[1]
Dosage:

1 mg/kg
Administration:

1 mg/kg, i.p.
Result:

Provided effective protection against TNFα-induced lethal shock.

Animal Model:

C57BL/6 mice^[1]
Dosage:

5 mg/kg
Administration:

5 mg/kg, i.v.
Result:

Significantly reduced the number of pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigration of RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate and invasion ability of B16-F10 or RFP-LL/2 cells without the endothelial cell monolayer in vitro.

Chemical Information

CAS. Nr. 2173556-69-7
Appearance Solid
Molecular Weight 424.52
Formel C₂₂H₂₄N₄O₃S
Color Off-white to light yellow
SMILES

O=C(OC1CCCCC1)NC2=CC(C3=CC=C4N=C(NC(C)=O)SC4=C3)=CN=C2C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 30 mg/mL (70.67 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

2.3556 mL

11.7780 mL

23.5560 mL

5 mM

0.4711 mL

2.3556 mL

4.7112 mL

10 mM

0.2356 mL

1.1778 mL

2.3556 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3 mg/mL (7.07 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

Verweise

[1]. Jue Hou, et al. Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis. Cell Death Dis. 2019 Jun 24;10(7):493. [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	2.3556 mL	11.7780 mL	23.5560 mL	58.8900 mL
	5 mM	0.4711 mL	2.3556 mL	4.7112 mL	11.7780 mL
	10 mM	0.2356 mL	1.1778 mL	2.3556 mL	5.8890 mL
	15 mM	0.1570 mL	0.7852 mL	1.5704 mL	3.9260 mL
	20 mM	0.1178 mL	0.5889 mL	1.1778 mL	2.9445 mL
	25 mM	0.0942 mL	0.4711 mL	0.9422 mL	2.3556 mL
	30 mM	0.0785 mL	0.3926 mL	0.7852 mL	1.9630 mL
	40 mM	0.0589 mL	0.2945 mL	0.5889 mL	1.4723 mL
	50 mM	0.0471 mL	0.2356 mL	0.4711 mL	1.1778 mL
	60 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9815 mL

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PK68

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PK68

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Protein-protein Interaction Inhibitor Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PK68 Related Classifications

HY-128348 Related Classifications