2. Epigenetics Membrane Transporter/Ion Channel
  3. WDR5 Potassium Channel
  4. HBI-2375

HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM.

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

HBI-2375

HBI-2375 Chemical Structure

CAS No. : 2982574-79-6

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 Customer Validation

HBI-2375 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM[1][2].

In Vitro

HBI-2375 inhibits the WDR5 WIN-site protein-protein interaction with an IC50 of 5 nM[1].
HBI-2375 reduces the viability of MV4:11 MLL-rearranged acute myeloid leukemia cells with a GI50 of 3200 nM[1].
HBI-2375 potently inhibits WDR5 in a cell-free biochemical assay with an IC50 of 4.48 nM[2].
HBI-2375 inhibits MV4-11 leukemia cell proliferation with an average IC50 of 3.17 µM in CTG assays[2].
HBI-2375 inhibits hERG in a cell-based assay with an IC50 of 17 µM[2].

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

HBI-2375 Related Antibodies
In Vivo

HBI-2375 exhibits dose-dependent antitumor activity in mouse models of acute myeloid leukemia (AML), enhances the antitumor efficacy of anti-PD-1 monoclonal antibodies in mouse models of colorectal cancer and lung cancer, and increases the infiltration of CD8+ cytotoxic T lymphocytes in tumor tissues[2].

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

616.11

Formula

C29H36ClF2N9O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C)C(F)=C(N)C=C1C(NC(C=C(N2C=C(C(N3CCN(C)CC3)=O)N=N2)C(F)=C4)=C4N5C[C@@H](C)N(C)[C@@H](C)C5)=O
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 : 20 mg/mL (32.46 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 1.6231 mL 8.1154 mL 16.2309 mL
5 mM 0.3246 mL 1.6231 mL 3.2462 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.

  • Molarity Calculator

  • Dilution Calculator

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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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 1.6231 mL 8.1154 mL 16.2309 mL 40.5772 mL
5 mM 0.3246 mL 1.6231 mL 3.2462 mL 8.1154 mL
10 mM 0.1623 mL 0.8115 mL 1.6231 mL 4.0577 mL
15 mM 0.1082 mL 0.5410 mL 1.0821 mL 2.7051 mL
20 mM 0.0812 mL 0.4058 mL 0.8115 mL 2.0289 mL
25 mM 0.0649 mL 0.3246 mL 0.6492 mL 1.6231 mL
30 mM 0.0541 mL 0.2705 mL 0.5410 mL 1.3526 mL
  • 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.

HBI-2375 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:

HBI-23752982574-79-6HYBI-084HBI2375HBI 2375HYBI084HYBI 084WDR5Potassium ChannelWD repeat protein-5WD40 repeat domain protein 5KcsAWIN-siteMLL1-WDR5 complexglioblastomaacute myeloid leukemiaMLL1 histone methyl transferaseMV4:11 MLL-rearranged acute myeloid leukemia cellsCD8+ cytotoxic T lymphocyteH3K4 methylationAML mouse modelsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
HBI-2375
Cat. No.:
HY-175802
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (254 KB) Français - FR (254 KB) Deutsch - DE (254 KB) Norwegian - NO (254 KB) Español - ES (254 KB) Swedish - SV (254 KB) Italian - IT (254 KB) Korean - KR (254 KB) Portuguese - PT (254 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.