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  3. Chetomin

Chetomin  (Synonyms: ケトミン)

製品番号: HY-107553 純度: 95.3%
COA 取扱説明書 Technical Support

Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule.

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Chetomin

Chetomin 構造式

CAS 番号 : 1403-36-7

容量 価格(税別) 在庫状況 数量
1 mg $489 在庫あり
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10 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

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製品説明

Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule[1].

IC50 & Target[1]

HSP90

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
3.5 3
Compound: 1
Cytotoxicity against human A549 cells assessed as inhibition of cell viability by MTT assay
Cytotoxicity against human A549 cells assessed as inhibition of cell viability by MTT assay
[PMID: 38888514]
B-cell IC50
0.09 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
B-cell IC50
0.09 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
T-cell IC50
0.17 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
T-cell IC50
0.17 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
B-cell IC50
0.09 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
HeLa IC50
2.4 3
Compound: 1
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability by MTT assay
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability by MTT assay
[PMID: 38888514]
T-cell IC50
0.17 6
Compound: 1, CS-A
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
体外実験

Chetomin (0~10 μM; 24 hours; H460 and H1299 cells) shows progressively lower expression of several survival-promoting proteins promoted by Hsp90/HIF1α activity, including insulin-like growth factor 1 (IGF1 R), epidermal growth factor receptor (EGFR), Src, mitogen-activated protein kinase kinase 1/2 (MEK1/2), activation of protein kinase B (Akt), and mammalian target of rapamycin (mTOR) [1].
Chetomin (0~10 μM; 24 hours; H1299 cells) elicits cell cycle arrest in susceptible and chemoresistant NSCLC cell lines[1].
. Chetomin (1 μM; 3 days; H460 and H1299 cells) pretreatment abolishes their sphere-forming capacity. Chetomin inhibits sphere-forming by NSCLC CSCs within a nanomolar range, and proliferation of susceptible and chemoresistant NSCLC non-CSCs within a micromolar range. Chetomin (24 h) decreases HIF-response element activity in H460 and H1299 monolayer cultures. Chetomin (0~10 μM) specifically inhibits the Hsp90-HIF1α binding interaction in HIF1α's N-terminus [1].

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

Western Blot Analysis[1]

Cell Line: H460 and H1299 cells
Concentration: 0~10 μM
Incubation Time: 24 hours
Result: Showed progressively lower expression of several survival-promoting proteins promoted by Hsp90/HIF1α activity, including insulin-like growth factor 1 (IGF1 R), epidermal growth factor receptor (EGFR), Src, mitogen-activated protein kinase kinase 1/2 (MEK1/2), activation of protein kinase B (Akt), and mammalian target of rapamycin (mTOR).

Cell Cycle Analysis[1]

Cell Line: H1299 cells
Concentration: 0~10 μM
Incubation Time: 24 hours
Result: Elicited cell cycle arrest in susceptible and chemoresistant NSCLC cell lines.
体内実験

Chetomin (0~100 mg/kg; p.o.) inhibits lung tumorigenesis in NSCLC mouse models[1].
Chetomin markedly decreases tumor formation in several murine models of NSCLC[1].

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

Animal Model: Mouse
Dosage: 0~100 mg/kg
Administration: P.o.
Result: Inhibited lung tumorigenesis in NSCLC mouse models.
分子量

710.87

分子式

C31H30N6O6S4

CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N2[C@]3([H])[C@](C4=CC=CC=C4N3)(N5C6=CC=CC=C6C(C[C@@]7(N8C)C(N([C@](SS7)(CO)C8=O)C)=O)=C5)C[C@]29C(N(C)[C@]1(SS9)CO)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 5 mg/mL (7.03 mM; Need ultrasonic and warming; 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 1.4067 mL 7.0336 mL 14.0673 mL
5 mM 0.2813 mL 1.4067 mL 2.8135 mL
10 mM --- --- ---
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.

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純度とドキュメンテーション

純度: ≥99.0%

参考文献

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 1.4067 mL 7.0336 mL 14.0673 mL 35.1682 mL
5 mM 0.2813 mL 1.4067 mL 2.8135 mL 7.0336 mL
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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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.

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製品名:
Chetomin
製品番号:
HY-107553
数量:
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