2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis
  3. ROR Apoptosis
  4. W6134

W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC).

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

W6134 Chemical Structure

W6134 Chemical Structure

CAS No. : 2983540-55-0

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Based on 1 publication(s) in Google Scholar

W6134 Related Antibodies

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Description

W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC)[1].

IC50 & Target

RORγ

0.21 μM (IC50)

In Vitro

W6134 (compound 29) has antiproliferative potencies on androgen receptor (AR)-positive human CRPC cell lines, including C4-2B, 22Rv1, and LNCaP, with IC50 values of 0.47 μM, 0.77 μM, and 0.63 μM, respectively[1].
W6134 (1.25-5 μM; 14 days) significantly suppresses the colony formation in C4-2B and 22Rv1 cell lines. W6134 dramatically induces apoptosis of C4-2B and 22Rv1 cells[1].
W6134 (1.25-5 μM; 48 h) inhibits the mRNA levels of AR-regulated genes, such as KLK2, KLK3, and NKX3-1[1].
W6134 (1.25-5 μM; 24-48 h) effectively suppresses the levels of AR or AR-V7 in a dose- and time-dependent manner[1].

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

W6134 Related Antibodies

Cell Migration Assay [1]

Cell Line: C4-2B and 22Rv1 cell lines
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 14 days
Result: Significantly suppressed the colony formation in C4-2B and 22Rv1 cell lines in a dose-dependent manner.

RT-PCR[1]

Cell Line: C4-2B and 22Rv1 cell lines
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Significantly decreased the expression of AR and its variant AR-V7 in a dose-dependent manner.
The mRNA levels of AR-regulated genes, such as KLK2, KLK3, and NKX3-1, were also dramatically suppressed.

Western Blot Analysis[1]

Cell Line: C4-2B and 22Rv1 cell lines
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Effectively suppressed the levels of AR or AR-V7 in a dose- and time-dependent manner.
In Vivo

W6134 (compound 29) (5-10 mg/kg; i.p; five times per week; for 2 weeks) markedly suppresseS the tumor growth in a 22Rv1 mouse tumor xenograft model[1].

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

Animal Model: Male NOD/SCID mice (~18 g; 4-week-old) were subcutaneously 22Rv1 cells[1]
Dosage: 5 mg/kg or 10 mg/kg
Administration: i.p; five times per week; for 2 weeks
Result: Significantly inhibited the tumor growth in a dose-dependent manner with tumor growth inhibition (TGI) values of 41.90 and 62.58% at doses of 5 and 10 mg/kg.
Molecular Weight

482.98

Formula

C25H23ClN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C2=C(C=CC=C2)NC(C=C)=O)C(Cl)=C1)CC3=CC=C(C=C3)S(=O)(CC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (172.53 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 2.0705 mL 10.3524 mL 20.7048 mL
5 mM 0.4141 mL 2.0705 mL 4.1410 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

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Volume (final)

V2

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

Dosage

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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 2.0705 mL 10.3524 mL 20.7048 mL 51.7620 mL
5 mM 0.4141 mL 2.0705 mL 4.1410 mL 10.3524 mL
10 mM 0.2070 mL 1.0352 mL 2.0705 mL 5.1762 mL
15 mM 0.1380 mL 0.6902 mL 1.3803 mL 3.4508 mL
20 mM 0.1035 mL 0.5176 mL 1.0352 mL 2.5881 mL
25 mM 0.0828 mL 0.4141 mL 0.8282 mL 2.0705 mL
30 mM 0.0690 mL 0.3451 mL 0.6902 mL 1.7254 mL
40 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2940 mL
50 mM 0.0414 mL 0.2070 mL 0.4141 mL 1.0352 mL
60 mM 0.0345 mL 0.1725 mL 0.3451 mL 0.8627 mL
80 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6470 mL
100 mM 0.0207 mL 0.1035 mL 0.2070 mL 0.5176 mL
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W6134 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:

W61342983540-55-0W 6134W-6134RORApoptosisRAR-related orphan receptorCRPC22Rv1 mouse tumor xenograft modelInhibitorinhibitorinhibit

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