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Ciliobrevin D Hedgehog/Smoothened inhibitor

Name: Ciliobrevin D
Brand: Selleck Chemicals
SKU: S9743
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S9743

Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. This compound perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.

Chemical Structure

Molecular Weight: 392.62

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Quality Control

Batch: S974301 DMSO]20 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.77%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.77

Related Targets	CXCR PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Other Hedgehog/Smoothened Inhibitors	SAG (Smoothened Agonist) Hydrochloride Purmorphamine Cyclopamine (11-Deoxojervine) GANT61 SAG (Smoothened Agonist) SANT-1 HPI-4 (Ciliobrevin A) BMS-833923 Taladegib (LY2940680) Jervine

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (50.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	392.62	Formula	C₁₇H₈Cl₃N₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1370554-01-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	ClC1=CC(=C(C=C1)C(=O)C(\C#N)=C2/NC(=O)C3=CC=C(Cl)C=C3N2)Cl

Mechanism of Action

Targets/IC₅₀/Ki	cytoplasmic dynein Hedgehog
In vitro	Ciliobrevin D inactivate dynein in Sertoli cells. The inactivation of dynein by this compound also perturbs gross disruption of F-actin across the Sertoli cells in vitro. It perturbs protein trafficking within the primary cilium, leading to their malformation and Hedgehog signaling blockade. This chemical also prevents spindle pole focusing, kinetochore-microtubule attachment, melanosome aggregation, and peroxisome motility in cultured cells.
In vivo	Ciliobrevin D inactivate dynein in the testis. The inactivation of dynein by this compound also perturbs gross disruption of F-actin across the seminiferous epithelium in vivo, illustrating there are cross talks between the two cytoskeletons in the testis.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22425997/ [2] https://pubmed.ncbi.nlm.nih.gov/30016153/

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