2. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  3. HDAC Apoptosis Histone Acetyltransferase Microtubule/Tubulin Caspase
  4. HDAC-IN-99

HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.

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

HDAC-IN-99

HDAC-IN-99 Chemical Structure

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HDAC-IN-99 Related Antibodies

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Description

HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer[1].

IC50 & Target[1]

HDAC1

48.09 nM (IC50)

HDAC2

300.28 nM (IC50)

HDAC6

9.16 nM (IC50)

In Vitro

HDAC-IN-99 (Z16) potently inhibits the activities of HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). It exhibits over 15-fold higher selectivity for HDAC6 than class I HDACs, while showing extremely low activity against HDAC8 (IC50 = 37.77 μM)[1].
HDAC-IN-99 inhibits the growth of various cancer cell lines, with IC50 values of 0.05 μM (HeLa), 0.07 μM (HCT116), 0.1 μM (SKOV3), 0.04 μM (MDA-MB-231) and 0.02 μM (Jurkat) against different cell lines[1].
HDAC-IN-99 (0-250 nM, 48 h) induces concentration-dependent S-phase cell cycle arrest and apoptosis in HCT116 cells, accompanied by increased acetylation levels of histone H3, histone H4 and α-tubulin, upregulated p21 expression, and cleavage of caspase-3[1].

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

HDAC-IN-99 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0, 40, 100, 250
Incubation Time: 48 h
Result: Induced concentration-dependent S-phase cell cycle arrest and apoptosis in HCT116 cells, accompanied by increased acetylation of histone H3, histone H4, and α-tubulin, upregulation of p21, and cleavage of caspase-3.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CL Vz AUC0-t AUC0-∞ F
Rat[1] 2 mg/kg i.v. 2880.00 ng/mL 0.08 h 1.28 h 1.45 L/h/kg 2.63 L/kg 1667.93 ng·h/mL 1750.26 ng·h/mL /
Rat[1] 20 mg/kg i.p. 2040.83 ng/mL 2.00 h 5.48 h 0.96 L/h/kg 7.24 L/kg 16130.71 ng·h/mL 17274.30 ng·h/mL 98.70 %
Mice[1] 2 mg/kg i.v. 1245.26 ng/mL 0.08 h 0.66 h 6.25 L/h/kg 5.77 L/kg 405.27 ng·h/mL 425.22 ng·h/mL /
Mice[1] 20 mg/kg i.p. 1248.09 ng/mL 1.40 h 1.25 h 4.83 L/h/kg 8.53 L/kg 4226.64 ng·h/mL 4092.64 ng·h/mL 96.25 %
In Vivo

HDAC-IN-99 (30-40 mg/kg, i.p., once daily) exhibits dose-dependent antitumor efficacy in the HCT116 colon cancer xenograft mice model[1].

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

Animal Model: BALB/c nude (female, 4-6 weeks old, SPF grade)[1]
Dosage: 30 mg/kg; 40 mg/kg
Administration: i.p.; q.d.
Result: Achieved a tumor growth inhibition (TGI) rate of 26.32%.
Achieved a tumor growth inhibition (TGI) rate of 45.80%.
Caused no significant changes in body weight during the study.
Molecular Weight

448.35

Formula

C23H25BN4O3S
SMILES

O=C(N[C@H](C1=NC=C(C2=CC3=C(C=C2)C=CC=C3)N1)CCCCCB(O)O)C4=CN=CS4
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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HDAC-IN-99 Related Classifications

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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.

Keywords:

HDAC-IN-99HDACApoptosisHistone AcetyltransferaseMicrotubule/TubulinCaspaseHistone deacetylasesHATsHAThistone deacetylase inhibitorcolon cancerHeLa cellsHCT116 cellsSKOV3 cellsMDA-MB-231cellsapoptosisBALB/c nude mice
Inhibitorinhibitorinhibit

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