2. PROTAC Apoptosis
  3. PROTACs RIP kinase
  4. PROTAC RIPK1 Degrader-1

PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373).

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

PROTAC RIPK1 Degrader-1

PROTAC RIPK1 Degrader-1 Chemical Structure

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PROTAC RIPK1 Degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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RIPK1 RIPK2 RIPK3

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Description

PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373)[1].

IC50 & Target[1]

VHL

 

RIPK1

 

In Vitro

PROTAC RIPK1 Degrader-1 (Compound 225-5) (0-1 μM, 1-20 h) induces RIPK1 degradation through the association of RIPK1, VHL, proteasome, and Cullin-RING E3 ligase complex in HEK-293T-RIPK1-HiBiT (DC50 < 0.1 nM, Dmax = 93 %), A375 (DC50 = 41 nM, Dmax = 97 %), B16F10 (DC50 = 91 nM, Dmax = 92 %), PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells[1].

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

PROTAC RIPK1 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: A375, B16F10, PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 1 h, 2 h, 4 h, 8 h, 16 h, 20 h
Result: Induced RIPK1 degradation.
In Vivo

PROTAC RIPK1 Degrader-1 (Compound 225-5) (10-50 mg/kg, i.p./i.v., twice daily/once daily, 3-11 days) lowers RIPK1 levels in B16F10 C57BL/6 mouse model [1].
PROTAC RIPK1 Degrader-1 (10-20 mg/kg, i.p., once daily, 3-11 days) lowers RIPK1 levels in humanized A375 melanoma NSG mouse model[1].

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

Animal Model: B16F10 (0.3 M) C57BL/6 mouse model[1]
Dosage: 50 mg/kg/10 mg/kg
Administration: i.p., twice daily, 3 days/i.v., twice daily, 3 days
Result: Lowered RIPK1 levels.
Animal Model: Humanized (PBMC, 1 × 107) A375 (5 M) melanoma NSG mouse model[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: i.p., once daily, 3 days
Result: Lowered RIPK1 levels.
Animal Model: B16F10 (0.3 M) syngeneic C57BL/6 mouse model[1]
Dosage: 40 mg/kg+20 mg/kg
Administration: i.p., once daily, 3 days+ once daily, 8 days
Result: Delayed tumor growth and extended median survival from 19 to 24 days when used in combination with radiation therapy.
Animal Model: A375 (1 M) humanized (PBMC, 1 × 107) NSG mouse model[1]
Dosage: 20 mg/kg
Administration: i.p., once daily, 11 days
Result: Reduced tumor volume by 89% in combination with radiation therapy.
Molecular Weight

1256.63

Formula

C69H85N13O6S2
SMILES

O=C(N1CCC(CC1)CN2CCC(CN3CCN(CC(N[C@H](C(N4[C@H](C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)CC3)CC2)CN7C=C(C=N7)C8=CN=C(N)C9=C8SC=C9C%10=CC=C%11N(C(CC%12=CC=CC=C%12)=O)CCC%11=C%10
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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PROTAC RIPK1 Degrader-1 Related Classifications

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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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:

PROTAC RIPK1 Degrader-1PROTACsRIP kinaseReceptor-interacting protein kinasesRIPKPROTACdegraderA375 cellsB16F10 cellsmelanomaNSG mouseInhibitorinhibitorinhibit

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