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Art. -Nr.: HY-N14094

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Tubulosine

Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC₅₀ value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC₅₀ values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells.

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CAS. Nr.: 2632-29-3
Formel: C₂₉H₃₇N₃O₃
Molecular Weight:475.62

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

Tubulosine Chemical Structure

CAS. Nr.: 2632-29-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[3]^[4]

JAK3

9.9 nM (IC₅₀)

JAK1

69.5 nM (IC₅₀)

JAK2

84.9 nM (IC₅₀)

Tyk2

76.3 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	ED₅₀	<1*10^-5 μg/mL Compound: 1	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 1982768]
A549	ED₅₀	1 10'-5μg/ml Compound: 1	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 1982768]
A549	IC₅₀	2.1 μM Compound: 12	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31513408]
BC1 cell line	ED₅₀	0.1 μg/mL Compound: 2	Cytotoxicity against human BC1 cells Cytotoxicity against human BC1 cells	[PMID: 10514334]
Col2	ED₅₀	0.05 μg/mL Compound: 2	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 10514334]
HeLa	IC₅₀	>10 μM Compound: 12	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31513408]
HT-29	ED₅₀	<1*10^-5 μg/mL Compound: 1	Cytotoxicity against human HT-29 cells Cytotoxicity against human HT-29 cells	[PMID: 1982768]
KB	ED₅₀	<0.16 μg/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 10514334]
KB	ED₅₀	0.1 μg/mL Compound: 2	Cytotoxicity against human multidrug resistant KB cells in absence of vinblastine Cytotoxicity against human multidrug resistant KB cells in absence of vinblastine	[PMID: 10514334]
LNCaP	ED₅₀	<0.16 μg/mL Compound: 2	Cytotoxicity against human LNCAP cells Cytotoxicity against human LNCAP cells	[PMID: 10514334]
Lu1	ED₅₀	<0.001 μg/mL Compound: 2	Cytotoxicity against human Lu1 cells Cytotoxicity against human Lu1 cells	[PMID: 10514334]
M109	ED₅₀	0.1 μg/mL Compound: 2	Cytotoxicity against mouse M109 cells Cytotoxicity against mouse M109 cells	[PMID: 10514334]
MCF7	ED₅₀	<1*10^-5 μg/mL Compound: 1	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 1982768]
SK-N-SH	ED₅₀	0.1 μg/mL Compound: 2	Cytotoxicity against human SK-N-SH cells Cytotoxicity against human SK-N-SH cells	[PMID: 10514334]
SK-OV-3	IC₅₀	0.4 μM Compound: 12	Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31513408]
SW626	ED₅₀	0.22 μg/mL Compound: 2	Cytotoxicity against human SW626 cells Cytotoxicity against human SW626 cells	[PMID: 10514334]

Chemical Information

CAS. Nr. 2632-29-3
Molecular Weight 475.62
Formel C₂₉H₃₇N₃O₃
SMILES

OC1=CC=C(N2)C(C(CCN3)=C2[C@H]3C[C@H]4C[C@@]5([H])C6=CC(OC)=C(OC)C=C6CCN5C[C@@H]4CC)=C1
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Brauchli P, et al. The structure of tubulosine, a novel alkaloid from Pogonopus tubulosus (DC.) Schumann. Journal of the American Chemical Society, 1964, 86(9): 1895-1896.

[2]. Carrasco L, et al. Specific inhibition of translocation by tubulosine in eukaryotic polysomes. Eur J Biochem. 1976 Apr 15;64(1):1-5. [Content Brief]

[3]. Kim BH , et al. Anticancer Activity of Tubulosine through Suppression of Interleukin-6-Induced Janus Kinase 2/Signal Transducer and Activation of Transcription 3 Signaling. J Breast Cancer. 2019 Sep;22(3):362-374. [Content Brief]

[4]. Kim BH, et al. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. J Cell Mol Med. 2020 Jul;24(13):7427-7438. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
Chemical Information
Reinheit & Dokumentation
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Tubulosine

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Tubulosine Related Classifications

HY-N14094 Related Classifications