1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. NHWD-870

NHWD-870 

Cat. No.: HY-134463 Purity: 99.36%
Handling Instructions

NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.

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

NHWD-870 Chemical Structure

NHWD-870 Chemical Structure

CAS No. : 2115742-03-3

Size Price Stock Quantity
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5000 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation[1].

In Vitro

NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM[1].
NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth[1].
NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation and c-MYC expression[1].
NHWD-870 exhibits mild inhibition of hERG channel (IC50 = 5.4 µM)[1]. NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation[1].

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

Cell Viability Assay[1]

Cell Line: H526, A2780, ES-2, and MDA-MB231 cells
Concentration: 0-10000 nM
Incubation Time: 5 days
Result: Showed strong inhibitory activities against these cells in 5-day assays.

Western Blot Analysis[1]

Cell Line: H526, A2780, ES-2, and MDA-MB231 cells
Concentration: 0-50 nM
Incubation Time: 24 hours
Result: Led to the depletion of phosphorylated BRD4 and c-MYC at 10 nM.
In Vivo

NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models[1].
NHWD-870 reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation[1].
NHWD-870 manifests diverse mechanisms of action in different cancer settings. These include: 1) inhibition of tumor cell growth by downregulating the PDGFRβ, MEK1/2 and STAT1/MYC signaling in tumor cells; 2) inhibition of tumor angiogenesis by decreasing PDGF production in tumor cells and the PDGFRβ and MEK1/2 signaling in endothelial cells. NHWD-870 has potent tumor suppressive efficacies in xenograft mouse models of small cell lung cancer, triple negative breast cancer and ovarian cancer[2].

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

Animal Model: 4-6 weeks old female BALB/c nude mice/6-8 weeks old female C57BL/6 mice were used for B16F10 experiments (bearing NCI-H526, A2780, A375, B16F10, and TMD-8 cells)[1]
Dosage: 0.75-3 mg/kg
Administration: P.o.; TMD8 and B16F10 melanoma model with once daily for 11-21 days; A375 melanoma and PDX of melanoma with once daily (5 days on, 2 days off) for 21 days.
Result: Strongly suppressed the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.
Molecular Weight

491.59

Formula

C₂₉H₂₉N₇O

CAS No.
SMILES

CN1N=CC2=CC3=C(N([[email protected]](C4=CC=CC=C4)C5CCOCC5)C6=CC(C7=C(C)N=NN7C)=CN=C63)C=C12

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (254.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0342 mL 10.1711 mL 20.3422 mL
5 mM 0.4068 mL 2.0342 mL 4.0684 mL
10 mM 0.2034 mL 1.0171 mL 2.0342 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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)
× = ×
C1   V1   C2   V2

Keywords:

NHWD-870NHWD870NHWD 870Epigenetic Reader DomainApoptosisoralselectivebromodomainscancercell-macrophageinteractionmelanomaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NHWD-870
Cat. No.:
HY-134463
Quantity:
MCE Japan Authorized Agent: