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

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.

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NHWD-870

NHWD-870 Chemische Struktur

CAS. Nr. : 2115742-03-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

NHWD-870 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE NHWD-870

  • Biologische Aktivität

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Beschreibung

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].

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
1.58 nM
Compound: 57; NHWD-870
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
[PMID: 37209450]
MDA-MB-231 IC50
1.58 nM
Compound: 5; NWHD-870
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability by MTS assay
[PMID: 36893627]
NCI-H211 IC50
1.99 nM
Compound: 57; NHWD-870
Antiproliferative activity against human NCI-H211 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H211 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
[PMID: 37209450]
NCI-H211 IC50
1.99 nM
Compound: 5; NWHD-870
Antiproliferative activity against human NCI-H211 cells assessed as reduction in cell viability by MTS assay
Antiproliferative activity against human NCI-H211 cells assessed as reduction in cell viability by MTS assay
[PMID: 36893627]
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].

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

NHWD-870 Related Antibodies

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].

MedChemExpress (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.
Klinische Studie
Molekulargewicht

491.59

Formel

C29H29N7O
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

CN1N=CC2=CC3=C(N([C@H](C4=CC=CC=C4)C5CCOCC5)C6=CC(C7=C(C)N=NN7C)=CN=C63)C=C12
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 62.5 mg/mL (127.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.36%

SDS (393 KB)

COA (261 KB) HNMR (219 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0342 mL 10.1711 mL 20.3422 mL 50.8554 mL
5 mM 0.4068 mL 2.0342 mL 4.0684 mL 10.1711 mL
10 mM 0.2034 mL 1.0171 mL 2.0342 mL 5.0855 mL
15 mM 0.1356 mL 0.6781 mL 1.3561 mL 3.3904 mL
20 mM 0.1017 mL 0.5086 mL 1.0171 mL 2.5428 mL
25 mM 0.0814 mL 0.4068 mL 0.8137 mL 2.0342 mL
30 mM 0.0678 mL 0.3390 mL 0.6781 mL 1.6952 mL
40 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2714 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0171 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8476 mL
80 mM 0.0254 mL 0.1271 mL 0.2543 mL 0.6357 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5086 mL
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NHWD-870 Related Classifications

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:

NHWD-8702115742-03-3NHWD870NHWD 870Epigenetic Reader DomainApoptosisoralselectivebromodomainscancercell-macrophageinteractionmelanomaInhibitorinhibitorinhibit

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