JX 06

Modify Date: 2024-01-12 10:15:07

JX 06 structure	Common Name	JX 06
	CAS Number	729-46-4	Molecular Weight	324.50600
	Density	1.463g/cm3	Boiling Point	466.3ºC at 760 mmHg
	Molecular Formula	C₁₀H₁₆N₂O₂S₄	Melting Point	N/A
	MSDS	N/A	Flash Point	235.8ºC

Use of JX 06

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with the IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity[1].

Name	morpholine-4-carbothioylsulfanyl morpholine-4-carbodithioate
Synonym	More Synonyms

Description	JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with the IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> PDHK Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer
Target	IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)[1]
In Vitro	JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM[1]. JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR[1]. JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells[1]. JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner[1]. JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells[1]. JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) [1]. Apoptosis Analysis[1] Cell Line: A549, EBC-1, HT-29 and H460 cells Concentration: 0, 1, 3, 10 μM Incubation Time: 48 hours Result: Induces cell apoptosis in A549 and EBC-1 cells. Cell Viability Assay[1] Cell Line: A549 cells Concentration: 0, 0.2, 0.4, 0.6 μM Incubation Time: 72 hours Result: Inhibits the viability of A549 cells in a dose dependent manner. Western Blot Analysis[1] Cell Line: A549 cells Concentration: 0, 0.1, 0.3, 1, 3, 10 μM Incubation Time: 0, 6, 12, 24 hours Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.
In Vivo	JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo[1]. Animal Model: A549 subcutaneous xenograft mice[1] Dosage: 40, 80 mg/kg Administration: I.p. injections for 21 days Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control. Well tolerated at the administration dose.
References	[1]. Wenyi S, et, al. JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. Cancer Res. 2015 Nov 15; 75(22): 4923-36.

Density	1.463g/cm3
Boiling Point	466.3ºC at 760 mmHg
Molecular Formula	C₁₀H₁₆N₂O₂S₄
Molecular Weight	324.50600
Flash Point	235.8ºC
Exact Mass	324.00900
PSA	139.72000
LogP	1.47780
Index of Refraction	1.69

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JO1530000

CHEMICAL NAME :: Disulfide, bis(morpholinothiocarbonyl)

CAS REGISTRY NUMBER :: 729-46-4

BEILSTEIN REFERENCE NO. :: 0276307

LAST UPDATED :: 199710

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C10-H16-N2-O2-S4

MOLECULAR WEIGHT :: 324.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 112,36,1957

Hazard Codes	Xn

DISULFIDE,BIS(MORPHOLINOTHIOCARBONYL)

Dimorpholinothiuramdisulfid

Disulfide,bis(4-morpholinylthioxomethyl)

Bis(morpholinothiocarbonyl) disulfide

Morpholine,4,4'-(dithiodicarbonothioyl)bis

Dimorpholinethiuram disulfide

Bis(4-morpholinothiocarbonyl) disulfide

N,N'-morpholinothiuram disulfide

4-Morpholinethiocarbonyl disulfide

bis(morpholinothiocarbonyl) disulphide

4,4'-(Dithiodicarbonothioyl)dimorpholine

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: JX 06
Price: Negotiable
Purity: 98.0%
Delivery: 10 Day
Contact: Huang
Email: sales@echemcloud.com

ShangHai DC Chemicals Co.,Ltd
China
Product Name: JX-06
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Lai
Email: order@dcchemicals.com

DC Chemicals Limited
China
Product Name: JX-06
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
Purity: 98.0%
Delivery: 3 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Morpholine,4,4'-(dithiodicarbonothioyl)bis-
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Delivery: Inquiry
Contact: Ms Wang
Email: enquiry@dycnchem.com

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