2. Apoptosis
  3. RIP kinase
  4. RIPK1-IN-11

RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity.

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RIPK1-IN-11 Chemical Structure

RIPK1-IN-11 Chemical Structure

CAS No. : 2173557-02-1

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RIPK1-IN-11 Related Antibodies

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Description

RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity[1].

Cellular Effect
Cell Line Type Value Description References
HT-29 EC50
17 nM
Compound: 70
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
30 nM
Compound: 70
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

RIPK1-IN-11 (compound 70) (24 hours; for 1h prior to the treatment of TNFα) efficiently blocks necroptosis induced by TNFα in both human and mouse cells (EC50=17-30 nM)[1].
Pharmacokinetic profiles of compound 70 in male SD rats

IV (2 mg/kg) PO (10 mg/kg)
Tmax (h) 1.2
Cmax (ng/mL) 1330 1241
AUC0-24 (ng/mL∗h) 1208 3827
t1/2 (ng/mL) 1.0 1.7
CL (mL/min/kg) 33
Vd, ss (L/kg) 2.4
F (%) 63%

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

RIPK1-IN-11 Related Antibodies
In Vivo

RIPK1-IN-11 (3 mg/kg; i.p. for 30 min, followed by injection with TNFα) blocks hypothermia and death in mice in the TNFα-induced SIRS model[1].
RIPK1-IN-11 (5 mg/kg, 25 mg/kg; p.o.; 7 days; C57BL/6 mouse) exhibits no obvious toxicity in mice[1].

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

Animal Model: C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome)[1]
Dosage: 3 mg/kg
Administration: i.p. for 30 min, followed by injection with TNFα (0.25 μg/g)
Result: Significantly reduced TNFα-induced temperature loss and ameliorated lethal shock in mice.
Molecular Weight

452.53

Formula

C23H24N4O4S
CAS No.
SMILES

O=C(OC1CCOCC1)NC2=CC(C3=CC=C4N=C(NC(C5CC5)=O)SC4=C3)=CN=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RIPK1-IN-11 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RIPK1-IN-112173557-02-1RIP kinaseReceptor-interacting protein kinasesRIPKnecroptosisRIPK1 kinaseinflammatoryTNFαanti-inflammatory activitytoxicityInhibitorinhibitorinhibit

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