2. Epigenetics
  3. WDR5
  4. WDR5-IN-5

WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

WDR5-IN-5

WDR5-IN-5 화학구조

CAS No. : 2417012-26-9

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
50 mg   견적 받기  
100 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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

고객리뷰

Based on 1 Customer Validation

WDR5-IN-5 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM[1].

IC50 & Target

Target: WIN site of WD repeat domain 5 (WDR5)[1]
In Vitro

WDR5 plays an important role in the activity of MLL1 histone methyltransferase (HMT) complexes. WDR5-IN-5 (compound 41), as a WDR5 inhibitor, will exihibits inhibitory effect towards HMT[1].
WDR5-IN-5 displays average soluble concentrations (kinetic solubility) of 60 μM[1].
WDR5-IN-5 exhibits high selectivity between K562 cells and MV4:11, the selectivity index (GI50, K562/GI50, MV4:11) is 290[1].
WDR5-IN-5 (0-30 μM; 5 d) inhibits cell proliferation of MV4:11, MOLM-13, and K562 with GI50 values are 13, 27, 3700 nM, respectively[1].

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

WDR5-IN-5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MV4:11, MOLM-13 cells
Concentration: 0-30 μM
Incubation Time: 5 days
Result: Inhibited cell growth of MV4:11, MOLM-13, and showed on- and off-target inhibition mechanism.
In Vivo

WDR5-IN-5 (compound 41) (10 mg/kg; p.o.) shows high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h[1].
WDR5-IN-5 (3 mg/kg; i.v.) also shows low iv clearance (26 mL/min/kg). WDR5-IN-5 is well tolerated and shows no adverse effects in mice by both i.v. and p.o. dosing[1].
WDR5-IN-5 can be formulated as 0.6 and 1 mg/mL solutions in ethanol, tocopherol poly (ethylene glycol) succinate (TPGS), PEG400 and water (v/v/v/v, 5/5/30/60) for i.v. and p.o. dosing, respectively[1].
PK profile of WDR5-IN-5 in CD-1 Mice[1]

Route Dose (mg/kg) CL (mL/min/kg) AUC0,inf (h.ng/mL) Vss (L/kg) T1/2 (h) F (%)
i.v. 3 26 1951 1.6 / /
p.o. 10 2083 3984 / 1.3 61

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

Animal Model: Male CD-1 mice[1]
Dosage: 3 mg/kg i.v.; 10 mg/kg p.o.
Administration: Intravenous injection or oral gavage
Result: Showed high oral exposure (AUC0,inf=3984 h.ng/mL), long half-life of T1/2=1.3 h, and low iv clearance (26 mL/min/kg).
분자량

534.58

화학식

C29H29F3N6O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N([C@@H](C2CC2)C3=NC=CC(C)=C3)CCC4=C1C=C(CN5C=CN=C5)C=C4C6=CN(CC)N=C6C(F)(F)F
선적

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

DMSO : 50 mg/mL (93.53 mM; Need ultrasonic; 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 1.8706 mL 9.3531 mL 18.7063 mL
5 mM 0.3741 mL 1.8706 mL 3.7413 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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: ≥ 1.25 mg/mL (2.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 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.
순도&문서
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 1.8706 mL 9.3531 mL 18.7063 mL 46.7657 mL
5 mM 0.3741 mL 1.8706 mL 3.7413 mL 9.3531 mL
10 mM 0.1871 mL 0.9353 mL 1.8706 mL 4.6766 mL
15 mM 0.1247 mL 0.6235 mL 1.2471 mL 3.1177 mL
20 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3383 mL
25 mM 0.0748 mL 0.3741 mL 0.7483 mL 1.8706 mL
30 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5589 mL
40 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1691 mL
50 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5846 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.

WDR5-IN-5 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:

WDR5-IN-52417012-26-9WDR5WD repeat protein-5WD40 repeat domain protein 5chromatinsmall molecule inhibitorribosomal proteinscancerMV4:11MOLM-13K562anti-proliferative activitypharmacokineticsWIN sitekinetic solubilityInhibitorinhibitorinhibit

최근 본 상품:

온라인 문의

Your information is safe with us. * Required Fields.

상품명

  

Requested Quantity *

고객명 *

 

호칭

메일주소 *

 

전화번호 *

Department

 

회사명 *

City

도

Country or Region *

      

비고

대량구매 문의

Inquiry Information

상품명:
WDR5-IN-5
Cat. No.:
HY-150654
수량:
MCE Japan Authorized Agent:

고객리뷰

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.

상품명

  

Lot #

고객명 *

 

메일주소 *

전화번호

 

Department *

회사명 *

 

Country or Region *

비고

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.