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5.00495

RubR1 Activator, GF-15

Synonym(s):

RubR1 Activator, GF-15, Supernumerary Centrosomes Clustering Inhibitor, 2ʹ-Benzyloxy-2ʹ-demethoxygriseofulvin, (2 S,6ʹ R)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1ʹ-(2ʹ-benzyloxy-6ʹ-methylcyclohex-2ʹ-en-4ʹ-one), (2, Supernumerary Centrosomes Clustering Inhibitor, 2ʹ-Benzyloxy-2ʹ-demethoxygriseofulvin, (2S,6ʹR)-(7-Chloro-4,6-dimethoxy-benzofuran-3-on)-2-spiro-1ʹ-(2ʹ-benzyloxy-6ʹ-methylcyclohex-2ʹ-en-4ʹ-one), (2S

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Size/SKUAvailabilityPrice
25 mg
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$263.00

About This Item

Empirical Formula (Hill Notation):
C23H21ClO6
CAS Number:
888042-13-5
Molecular Weight:
428.86
MDL number:
MFCD28963906
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$263.00

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assay

≥98% (HPLC)

Quality Segment

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

General description

A cell-permeable 2′-benzyloxy griseofulvin derivative that displays enhanced mammalian cancer-selective toxicity (IC50 ≤2, ≤4, ≤12, and ≥30 µM against panels of leukemia, myeloma, solid tumors, and non-malignant cell lines, respectively), but little antifungal activity, by activating spindle-assembly-checkpoint (Pos. vs. Neg. RubR1 staining of metaphase PC-3 kinetophores with or without 24 h 0.75 µM GF-15 treatment) without affecting microtubule kinetochore attachment (Neg. Mad2 staining of metaphase PC-3 kinetophores with or without GF-15). Cancer cells are reported to undergo multipolar (MP) mitosis with normal or supernumerary centrosomes (Aberrant vs. declustered, respectively) in the presence of GF-15 (%Declustered / %Aberrant MP mitotic cells among all anaphase cells = 5.6/&lt0.5, 10/3.9, 16/18, 28/30, respectively, in PC-3 cultures treated with 0, 0.375, 0.75, or 1.5 µM GF-15 for 24 h), resulting in subsequent apoptotic cell death. Shown to retard OPM2 myeloma- and HT29 colon cancer-derived tumor expansion in mice (by 49% and 56%, respectively at the end of 2-wk treatment; 10 i.p. dosages at 20 mg/kg/day in 2 weeks) in vivo. Based on stability data obtained with its p-iodobenzyl analogue, GF-15 half-life is expected to be least 48 h in cultures.

Biochem/physiol Actions

Cell permeable: yes
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Raab, M.S., et al. 2012. Cancer Res.72, 5374.
Ronnest, M.H., et al. 2009. J. Med. Chem.52, 3342.
Crosse, R., et al. 1964. J. Gen. Microbiol.34, 51.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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CDC25 Phosphatase Inhibitor I, BN82002 The CDC25 Phosphatase Inhibitor I, BN82002, also referenced under CAS 396073-89-5, controls the biological activity of CDC25 Phosphatase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

217691

CDC25 Phosphatase Inhibitor I, BN82002

STING Agonist, 2′3′-cGAMP

Sigma-Aldrich

531889

STING Agonist, 2′3′-cGAMP

description

-

description

-

description

The CDC25 Phosphatase Inhibitor I, BN82002, also referenced under CAS 396073-89-5, controls the biological activity of CDC25 Phosphatase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

description

-

form

solid

form

powder

form

solid

form

solid

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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