2. Epigenetics
    Apoptosis
  3. Histone Methyltransferase
    Apoptosis
  4. WDR5-IN-1

WDR5-IN-1 

Cat. No.: HY-133121 Purity: 98.71%
COA Handling Instructions

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

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

WDR5-IN-1 Chemical Structure

WDR5-IN-1 Chemical Structure

CAS No. : 2408842-51-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 566 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 566 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 880 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].

In Vitro

WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].
WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1]. WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM[1].

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

Cell Cycle Analysis[1]

Cell Line: MV4:11 cells
Concentration: 1 µM
Incubation Time: 48 hours
Result: Showed an approximate 4 fold increased SubG1 cells.

Western Blot Analysis[1]

Cell Line: MV4:11 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time: 24, 48 hours
Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.
Molecular Weight

514.59

Appearance

Solid

Formula

C30H31FN4O3
CAS No.
SMILES

COC1=CC(OC)=CC(CN2C(C(C=C(CN3C(N(C)C=C3)=N)C=C4C5=C(C)C=C(F)C=C5)=C4CC2)=O)=C1
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 : 100 mg/mL (194.33 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9433 mL 9.7165 mL 19.4329 mL
5 mM 0.3887 mL 1.9433 mL 3.8866 mL
10 mM 0.1943 mL 0.9716 mL 1.9433 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: ≥ 2.5 mg/mL (4.86 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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Keywords:

WDR5-IN-12408842-51-1Histone MethyltransferaseApoptosisMYCproliferativelymphomaneuroblastomaapoptosiscycleturmorigenesischromatin,Inhibitorinhibitorinhibit

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