country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-188392

Copy Link Print Information

KWGS-B11

KWGS-B11 is a selective VHL-recruiting RIPK1 PROTAC degrader with a K_d of 1.29 nM and a DC₅₀ of 4.48 nM. KWGS-B11 induces RIPK1 ubiquitination and proteasomal degradation. KWGS-B11 sensitizes cells to TNF-alpha-triggered cell death. KWGS-B11 enhances the antitumor efficacy of anti-PD-1 immunotherapy in a mouse melanoma model.
(Pink: RIPK1 ligand (HY-188393); Blue: VHL ligand (HY-112078); Black: linker (HY-188394)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₆₅H₇₄N₁₀O₇S
Molecular Weight:1139.41

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

KWGS-B11 Chemical Structure

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

KWGS-B11 is a selective VHL-recruiting RIPK1 PROTAC degrader with a K_d of 1.29 nM and a DC₅₀ of 4.48 nM. KWGS-B11 induces RIPK1 ubiquitination and proteasomal degradation. KWGS-B11 sensitizes cells to TNF-alpha-triggered cell death. KWGS-B11 enhances the antitumor efficacy of anti-PD-1 immunotherapy in a mouse melanoma model^[1]. (Pink: RIPK1 ligand (HY-188393); Blue: VHL ligand (HY-112078); Black: linker (HY-188394)).

IC₅₀ & Target

^[1]

RIPK1

4.48 nM (DC₅₀)

VHL

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	DC₅₀	4.48 nM	DC50 for RIPK1 degradation in human A375 melanoma cells assessed by dose-response Western blot analysis. DC50 for RIPK1 degradation in human A375 melanoma cells assessed by dose-response Western blot analysis.	42833023
B16-F10	DC₅₀	4.61 nM	DC50 for RIPK1 degradation in mouse B16F10 melanoma cells assessed by dose-response Western blot analysis. DC50 for RIPK1 degradation in mouse B16F10 melanoma cells assessed by dose-response Western blot analysis.	42833023

In Vitro

Anti-cancerCytokines & ChemokinesProtein/Amino Acid MetabolismApoptosisOthers

Anti-cancer

KWGS-B11 (0.1-1000 nM; 24 h) promotes RIPK1-VHL colocalization and depletes RIPK1 fluorescence in B16F10 cells, with near-complete loss at 100 nM^[1].

Anti-cancer

Cytokines & Chemokines

KWGS-B11 (1 μM; 24 h) enhances TNF-α-mediated cytotoxicity in B16F10 melanoma cells, producing marked viability loss in combination^[1].
KWGS-B11 (1 μM; 0-24 h) moderately suppresses B16F10 migration alone and significantly enhances TNF-α-mediated inhibition of migration in combination^[1].

Anti-cancer

Protein/Amino Acid Metabolism

KWGS-B11 potently degrades RIPK1 in A375 and B16F10 melanoma cells with DC₅₀ values of 4.48 nM and 4.61 nM, respectively, and 98% maximum degradation^[1].
KWGS-B11 (1 μM; 0-48 h) induces rapid and durable RIPK1 depletion in B16F10 cells, beginning by 2 h and persisting through 48 h^[1].

Apoptosis

Anti-cancer

Cytokines & Chemokines

KWGS-B11 (1 μM; 24 h) sensitizes B16F10 melanoma cells to TNF-α-induced apoptosis^[1].

Protein/Amino Acid Metabolism

KWGS-B11 degrades RIPK1 in B16F10 cells through a VHL-dependent ubiquitin-proteasome mechanism rather than the lysosomal pathway^[1].

Others

KWGS-B11 binds RIPK1 directly with a K_D of 1.29 nM in cell-free SPR^[1].

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

Western Blot Analysis^[1]

Cell Line:

B16F10 melanoma cells
Concentration:

1 μM
Incubation Time:

0, 2, 4, 8, 12, 24, and 48 h
Result:

Initiated obvious RIPK1 downregulation at 2 h, reached maximal degradation at 8 h, and sustained potent RIPK1 depletion for at least 48 h without apparent RIPK1 recovery.

Immunofluorescence^[1]

Cell Line:

B16F10 melanoma cells
Concentration:

0.1, 1, 10, 100, and 1000 nM
Incubation Time:

24 h
Result:

Promoted intracellular colocalization of RIPK1 and VHL in a concentration-dependent manner and gradually ablated endogenous RIPK1 fluorescence; at 100 nM, the RIPK1 signal was almost completely abolished.

Apoptosis Analysis^[1]

Cell Line:

B16F10 melanoma cells
Concentration:

1 μM (KWGS-B11); 100 ng/mL (TNF-α)
Incubation Time:

24 h
Result:

Showed no pro-apoptotic effect alone.
Combination with TNF-α triggered robust B16F10 melanoma cell apoptosis.

Cell Viability Assay^[1]

Cell Line:

B16F10 melanoma cells
Concentration:

1 μM (KWGS-B11); 100 ng/mL (TNF-α)
Incubation Time:

24 h
Result:

Showed minimal cytotoxicity alone.
Combination with TNF-α markedly reduced B16F10 cell viability compared with single agents.

Cell Migration Assay^[1]

Cell Line:

B16F10 melanoma cells
Concentration:

1 μM (KWGS-B11); 100 ng/mL (TNF-α)
Incubation Time:

0 and 24 h
Result:

Moderately suppressed B16F10 migration.
Combination with TNF-α significantly inhibited cell migration compared with individual monotherapies.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-t	T_1/2
Rat^[1]	5 mg/kg	i.p.	40.90 μg/L	2.83 h	327.58 μg/L·h	4.01 h

In Vivo

Anti-cancerImmune Tolerance & Immunosuppression

Anti-cancer

KWGS-B11 (40 μg; intratumoral; every 2 days) alone does not inhibit B16F10 tumor growth in C57BL/6J mice, but combined with MSA-2 achieves 69.1% tumor growth inhibition^[1].

Anti-cancer

Immune Tolerance & Immunosuppression

KWGS-B11 (40 μg; intratumoral; every 2 days) alone does not inhibit B16F10 tumor growth in C57BL/6J mice, but combined with anti-PD-1 achieves 83.7% tumor growth inhibition^[1].

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

Animal Model:

C57BL/6J (female)^[1]
Dosage:

40 μg per dose (KWGS-B11); 100 μg per dose (anti-PD-1)
Administration:

intratumoral (KWGS-B11); every 2 days; intraperitoneal (anti-PD-1); every 3 days
Result:

Did not inhibit tumor growth.
Combination with anti-PD-1 achieved a tumor growth inhibition (TGI) of 83.7% and reduced tumor weight.

Animal Model:

C57BL/6J (female)^[1]
Dosage:

40 μg per dose (KWGS-B11); 15 mg/kg (MSA-2)
Administration:

intratumoral (KWGS-B11); every 2 days; intraperitoneal (MSA-2); every 3 days
Result:

Did not show inhibition of tumor growth.
Combination with MSA-2 achieved a tumor growth inhibition (TGI) of 69.1%.

Related Protocols :

Chemical Information

Molecular Weight 1139.41
Formel C₆₅H₇₄N₁₀O₇S
SMILES

O=C(C1=C(CC2=CC=CC=C2)N(C)N=C1)NCC(C=C3)=CC=C3N4C5=CC=C(C(NCCCCCCOC6=CC=C(CCC(N[C@@H](C(C)(C)C)C(N7[C@H](C(N[C@H](C8=CC=C(C9=C(C)N=CS9)C=C8)C)=O)C[C@@H](O)C7)=O)=O)C=C6)=O)C=C5N=C4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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]. Guo S, et al. Targeting the nonenzymatic scaffold function of RIPK1 via a VHL-recruiting PROTAC synergizes with immunotherapy in melanoma. Eur J Med Chem. 2026 Sep 29;321(Pt 1):119359.

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

KWGS-B11

Biologische Aktivität

Beschreibung

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

KWGS-B11 Related Classifications

HY-188392 Related Classifications

Bioz

Keywords

Your Recently Viewed Products

IC₅₀ & Target