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C0621

Sigma-Aldrich

CI−994

≥98% (HPLC), powder

Synonym(e):

4-Acetylamino-N-(2′-aminophenyl)benzamide, Acetyldinaline, Tacedinaline

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About This Item

Empirische Formel (Hill-System):
C15H15N3O2
CAS-Nummer:
112522-64-2
Molekulargewicht:
269.30
MDL-Nummer:
MFCD00866266
UNSPSC-Code:
12352200
PubChem Substanz-ID:
329774808
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

off-white

Löslichkeit

DMSO: >10 mg/mL

Lagertemp.

room temp

SMILES String

CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N

InChI

1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20)

InChIKey

VAZAPHZUAVEOMC-UHFFFAOYSA-N

Angaben zum Gen

human ... HDAC1(3065) , HDAC10(83933) , HDAC11(79885) , HDAC2(3066) , HDAC3(8841) , HDAC4(9759) , HDAC5(10014) , HDAC6(10013) , HDAC7(51564) , HDAC8(55869) , HDAC9(9734)

Anwendung

CI-994 has been used:
  • as an histone deacetylase (HDAC) inhibitor to treat SUM229 and DT22 cells to study its effects
  • as an HDAC inhibitor for screening in SPEL cells
  • to study its effects on human myeloid and erythroid progenitors

Biochem./physiol. Wirkung

CI-994 is the acetylated derivative form of the original compound Dinaline (PD 104 208). It is an oral cytostatic drug with impressive differential activity against leukemic cells & normal stem-cells. It is used for combination therapy for selected tumors including non-small cell lung, pancreatic, breast, and colorectal cancers. It acts as a histone deacetylase inhibitor. CI-994 blocks cells in the G1-S phase of the cell cycle. The 16 kDa phosphoprotein is confined to the nuclear compartment. Loss of the 16-kDa nuclear phosphoprotein appears to be a direct effect of CI-994 treatment and that the inhibition of this phosphoprotein may play a critical role in the mechanism of action of CI-994.

Leistungsmerkmale und Vorteile

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Piktogramme

Exclamation mark
GHS07

Signalwort

Warning

H-Sätze

H319

Gefahreneinstufungen

Eye Irrit. 2

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

dust mask type N95 (US), Eyeshields, Gloves

Analysenzertifikate (COA)

Suchen Sie nach Analysenzertifikate (COA), indem Sie die Lot-/Chargennummer des Produkts eingeben. Lot- und Chargennummern sind auf dem Produktetikett hinter den Wörtern ‘Lot’ oder ‘Batch’ (Lot oder Charge) zu finden.

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Trichostatin A ≥98% (HPLC), from Streptomyces sp.

Sigma-Aldrich

T8552

Trichostatin A

5-Azacytidin ≥98% (HPLC)

Sigma-Aldrich

A2385

5-Azacytidin

5-Aza-2′-Desoxycytidin ≥97%

Sigma-Aldrich

A3656

5-Aza-2′-Desoxycytidin

Valproinsäure Natriumsalz 98%

Sigma-Aldrich

P4543

Valproinsäure Natriumsalz

CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies
Fuller NO, et al.
ACS Chemical Neuroscience (2019)
D A Richards et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 17(7), 1096-1102 (2006-04-28)
CI-994, an oral histone deacetylase inhibitor, has antineoplastic activity and synergism with gemcitabine preclinically. This randomized phase II trial explored whether CI-994 plus gemcitabine improves overall survival, objective response, duration of response, time to treatment failure and change in quality
M H Seelig et al.
European journal of cancer (Oxford, England : 1990), 32A(11), 1968-1976 (1996-10-01)
Dinaline [4-amino-N-(2'-aminophenyl)-benzamide, Din], p-N-methyldinaline (Me-Din) and p-N-acetyldinaline (Ac-Din) were evaluated for their antineoplastic efficacy in acetoxymethylmethylnitrosamine-induced colorectal carcinomas in Sprague-Dawley rats and in two human colon cancer cell lines. Din was very effective at all dosages (10, 7.7 and 5.9
H M el-Beltagi et al.
Leukemia, 7(11), 1795-1800 (1993-11-01)
The efficacy of acetyldinaline [4-acetylamino-N-(2'-aminophenyl)-benzamide] for eradication of minimal residual disease (MRD), which is left after bone marrow transplantation, and the risk of a bone marrow graft being jeopardized by this treatment was studied in the Brown Norway rat acute
S Prakash et al.
Investigational new drugs, 19(1), 1-11 (2001-04-09)
CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts. While cytotoxic in the Brown Norway (BN) rat leukemia model, growth inhibition in other murine and human tumor xenografts
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