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.

For research use only. We do not sell to patients.

JNJ-16241199 Chemical Structure

JNJ-16241199 Chemical Structure

CAS No. : 604769-01-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 361 In-stock
Solution
10 mM * 1 mL in DMSO USD 380 In-stock
Solid
1 mg USD 138 In-stock
5 mg USD 345 In-stock
10 mg USD 552 In-stock
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Based on 1 publication(s) in Google Scholar

JNJ-16241199 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 11.67 mg/mL (28.23 mM; ultrasonic and warming and heat to 60°C; 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 2.4187 mL 12.0934 mL 24.1867 mL
5 mM 0.4837 mL 2.4187 mL 4.8373 mL
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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Purity & Documentation

Purity: 99.05%

Data Sheet (273 KB) SDS (393 KB)

COA (247 KB) HNMR (117 KB) RP-HPLC (145 KB) LCMS (166 KB)

Handling Instructions (2659 KB)
References

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 2.4187 mL 12.0934 mL 24.1867 mL 60.4668 mL
5 mM 0.4837 mL 2.4187 mL 4.8373 mL 12.0934 mL
10 mM 0.2419 mL 1.2093 mL 2.4187 mL 6.0467 mL
15 mM 0.1612 mL 0.8062 mL 1.6124 mL 4.0311 mL
20 mM 0.1209 mL 0.6047 mL 1.2093 mL 3.0233 mL
25 mM 0.0967 mL 0.4837 mL 0.9675 mL 2.4187 mL
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JNJ-16241199 Related Classifications

Keywords:

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

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