2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Apoptosis HDAC
  4. JNJ-16241199

JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.

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JNJ-16241199 Chemical Structure

JNJ-16241199 Chemical Structure

CAS No. : 604769-01-9

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JNJ-16241199 Related Antibodies

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Description

JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study[1].

IC50 & Target

HDAC1

3.3 nM (IC50)

HDAC8

23 nM (IC50)

In Vitro

JNJ-16241199 (R306465) (10-40 mpk/day for 28 days, p.o.) inhibits the growth of A2780 ovarian, H460 lung and HCT116 colon carcinomas orthotopic xenograft tumor models [1].

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

JNJ-16241199 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 0, 0.1, 0.3, 1 μM
Incubation Time: 24 h or 48 h
Result: Decreased in S phase at 300 nM, with a parallel increase in G1 phase, but increased in the sub-G1 fraction of cells at the 1 μM after 24 h.
Increased in sub-G1 phase at all active concentrations starting from 100 nM after 48 h.
In Vivo

JNJ-16241199 (R306465) inhibits proliferation in acute lymphoblastic leukaemia (ALL), AML, chronic lymphoblastic leukaemia (CLL), chronic myeloid leukaemia (CML), lymphoma and myeloma tumour cells (IC50 values = 15–486 nM) [1].
JNJ-16241199 inhibits the primary human mammary epithelial cell (HMEC) proliferation with the IC50 of 32 nM, and is insensitive to quiescent, non-proliferative HMEC cells (IC50 = 7815 nM) [1].
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) induces apoptosis and inhibits angiogenesis in A2780 cell line[1].

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

Animal Model: Human A2780, H460 and HCT116 orthotopic xenograft tumor models[1]
Dosage: 10-40 mpk/day for 28 days
Administration: Oral gavage (p.o.)
Result: Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue.
Decreased tumour volume in three orthotopic xenograft tumor models.
Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
Molecular Weight

413.45

Formula

C19H19N5O4S
CAS No.
SMILES

O=S(N(CC1)CCN1C2=NC=C(C(NO)=O)C=N2)(C3=CC=C4C(C=CC=C4)=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JNJ-16241199 Related Classifications

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  • 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.

Keywords:

JNJ-16241199604769-01-9R306465JNJ16241199JNJ 16241199R 306465R-306465ApoptosisHDACHistone deacetylasesA2780H460T116Acute lymphoblastic leukaemiaChronic lymphoblastic leukaemiaChronic myeloid leukaemiaLymphoma and myelomaInhibitorinhibitorinhibit

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