Cat. No.: HY-N2600

Kuwanon H

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Based on 1 Customer Validation

Kuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a K_i value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA₂ and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A₂ generation and integrin αIIb/β₃ activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.

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

Purity: 98.0%
CAS No.: 76472-87-2
Formula: C₄₅H₄₄O₁₁
Molecular Weight:760.82

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Kuwanon H Chemical Structure

CAS No.: 76472-87-2

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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
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

GRP-R

290 nM (Ki)

NMB-R

6500 nM (Ki)

All Akt Isoforms :

All mTOR Isoforms :

All ERK Isoforms :

All p38 MAPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	2.4 x 10^-5 M Compound: kumanon H	Inhibition of 12-hydroxy-5,8,10-heptadecatrienoic acid formation in Wistar King platelets Inhibition of 12-hydroxy-5,8,10-heptadecatrienoic acid formation in Wistar King platelets	[PMID: 3097265]
Platelet	IC₅₀	7.57 x 10^-5 M Compound: kumanon H	Inhibition of thromboxane B2 formation in Wistar King platelets Inhibition of thromboxane B2 formation in Wistar King platelets	[PMID: 3097265]

In Vitro

Kuwanon H (30 μM; 48 h) induces apoptosis in A375 and MV3 melanoma cells^[1].
Kuwanon H (60 min) competitively inhibits the binding of [¹²⁵I]GRP to GRP-preferring receptors in mouse Swiss 3T3 fibroblasts with a K_i value of 290 nM, while showing no off-target binding to endothelin-1 or neuropeptide Y receptors at a concentration of 1 μM^[2].
Kuwanon H inhibits the binding of [¹²⁵I]bombesin to NMB-preferring receptors in rat esophageal membranes, with a K_i value of 6500 nM, indicating that its potency against NMB-Rs is 22.4-fold lower than that against GRP-Rs^[2].
Kuwanon H (500 nM; administered 1 min prior to agonist stimulation) reduces the bradykinin-induced elevation of cytosolic free calcium by 60% in mouse Swiss 3T3 fibroblasts, without altering basal calcium levels or cellular responses to endothelin-1 and bradykinin^[2].
Kuwanon H inhibits GRP-induced DNA synthesis in mouse Swiss 3T3 fibroblasts, with an IC₅₀ of approximately 100 nM^[2].
Kuwanon H (75-200 μM; 2 min pre-incubation, 7 min aggregation monitoring) inhibits Collagen (HY-NP003)-induced platelet aggregation in a concentration-dependent manner without inducing cytotoxicity^[3].
Kuwanon H (75-200 μM; 5 min) inhibits collagen-induced intracellular calcium mobilization in platelets by regulating InsP₃R and ERK phosphorylation^[3].
Kuwanon H (75-200 μM; 2 min pre-incubation, 7 min aggregation monitoring) inhibits collagen-induced secretion of 5-hydroxytryptamine and ATP from dense granules in platelets^[3].
Kuwanon H (75-200 μM; 2 min pre-incubation, 7 min aggregation monitoring) inhibits collagen-induced TXA₂ production in platelets by reducing the phosphorylation levels of cPLA₂ and p38^[3].
Kuwanon H (75-200 μM; 2 min incubation, 20 min adhesion incubation) inhibits Collagen-induced fibronectin adhesion in human platelets^[3].
Kuwanon H (75-200 μM; 1 min incubation, 25 min clot retraction monitoring) inhibits integrin αIIb/β₃ activity by regulating the phosphorylation of Akt and VASP, thereby delaying thrombin-induced fibrin clot retraction in human platelet-rich plasma (PRP)^[3].

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

Apoptosis Analysis^[1]

Cell Line:

A375, MV3 melanoma cells
Concentration:

30 μM (Kuwanon H); 5 mM (3-MA (HY-19312), preincubation)
Incubation Time:

48 h (Kuwanon H); 6 h (3-MA, preincubation)
Result:

Induces apoptosis in A375 and MV3 melanoma cells.
Reduced apoptosis rates to ~12% from ~18% in A375 cells relative to Kuwanon H alone.
Reduced apoptosis rates to ~10% from ~15% in MV3 cells relative to Kuwanon H alone.
Suppressed Kuwanon H-induced upregulation of cleaved caspase-3 and cleaved PARP in both cell lines.

In Vivo

Kuwanon H (50 mg/kg; once every 2 days; for 2 weeks) significantly inhibits melanoma tumor growth in vivo, as evidenced by reduced tumor weight and volume, decreased cell proliferation, and induced apoptosis via blocking autophagic flux; in addition, its combination with CDDP (HY-17394) enhances the anti-melanoma efficacy^[1].

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

Animal Model:

BALB/c null mice (4 weeks old, acclimated for 1 week prior to experimentation)^[1]
Dosage:

50 mg/kg (single-agent); 50 mg/kg (in combination with 25 mg/kg CDDP)
Administration:

s.c.; every 2 days; 2 weeks
Result:

Reduced tumor size, volume, and weight significantly compared to vehicle control.
Decreased Ki67-positive proliferating cells to ~30% (from ~95% in vehicle controls).
Increased TUNEL-positive apoptotic cells to ~20% (from <5% in vehicle controls).
Increased LC3B and SQSTM1 levels in tumor tissues, indicating impaired autophagy flux.
Enhanced tumor volume and weight reduction significantly when combined with CDDP compared to either single-agent treatment.
Reduced Ki67-positive proliferating cells to ~15% in combination with CDDP.
Increased TUNEL-positive apoptotic cells to ~40% in combination with CDDP.
Further accumulated LC3B and SQSTM1 levels in tumor tissues compared to CDDP alone.

Chemical Information

CAS No. 76472-87-2
Appearance Solid
Molecular Weight 760.82
Formula C₄₅H₄₄O₁₁
Color Yellow to orange
SMILES

OC1=CC(O)=C(C(C(C/C=C(C)/C)=C(C2=C(C=C(O)C=C2)O)O3)=O)C3=C1[C@@H]4[C@H]([C@H](C5=C(C=C(O)C=C5)O)CC(C)=C4)C(C6=C(C(C/C=C(C)/C)=C(O)C=C6)O)=O
Structure Classification
- Flavonoids
- Flavones
- Phenols
- Polyphenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (131.44 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

1.3144 mL

6.5719 mL

13.1437 mL

5 mM

0.2629 mL

1.3144 mL

2.6287 mL

10 mM

0.1314 mL

0.6572 mL

1.3144 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 (protect from light). 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)

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Molecular Weight Molecular Weight

Dilution Calculator

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

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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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

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

Solubility: ≥ 2.5 mg/mL (3.29 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Hu X, et al. Kuwanon H Inhibits Melanoma Growth through Cytotoxic Endoplasmic Reticulum Stress and Impaired Autophagy Flux. Journal of agricultural and food chemistry. 2023 Sep 20;71(37):13768-13782. [Content Brief]

[2]. Mihara S, et al. Non-peptide bombesin receptor antagonists, kuwanon G and H, isolated from mulberry. Biochemical and biophysical research communications. 1995 Aug 15;213(2):594-9. [Content Brief]

[3]. Shin, et al. Inhibition of Platelet Aggregation and Clot Retraction by Kuwanon H. Biomedical Science Letters, 32(2), 184-191.

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.3144 mL	6.5719 mL	13.1437 mL	32.8593 mL
	5 mM	0.2629 mL	1.3144 mL	2.6287 mL	6.5719 mL
	10 mM	0.1314 mL	0.6572 mL	1.3144 mL	3.2859 mL
	15 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1906 mL
	20 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6430 mL
	25 mM	0.0526 mL	0.2629 mL	0.5257 mL	1.3144 mL
	30 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	40 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8215 mL
	50 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6572 mL
	60 mM	0.0219 mL	0.1095 mL	0.2191 mL	0.5477 mL
	80 mM	0.0164 mL	0.0821 mL	0.1643 mL	0.4107 mL
	100 mM	0.0131 mL	0.0657 mL	0.1314 mL	0.3286 mL

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Kuwanon H

Apoptosis Compound Library

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