2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Apoptosis Caspase
  4. HDAC-IN-94

HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3, 10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.

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HDAC-IN-94

HDAC-IN-94 Chemical Structure

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HDAC-IN-94 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

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

View All Caspase Isoform Specific Products:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3, 10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research[1].

IC50 & Target[1]

hHDAC6

4.5 nM (IC50)

hHDAC8

3273 nM (IC50)

hHDAC1

403 nM (IC50)

hHDAC10

202 nM (IC50)

hHDAC2

537 nM (IC50)

hHDAC3

1278 nM (IC50)

hHDAC5

4455 nM (IC50)

hHDAC11

>10000 nM (IC50)

In Vitro

HDAC-IN-94 (compound 5o) fits within the catalytic site of hHDAC6 with the hydroxamic acid group, modelled in neutral form, able to chelate the zinc atom, and its polar benzamide hydrogen forming a hydrogen bond with Ser568[1].
HDAC-IN-94 (1-10 μM, 24 h) promotes acetylation of α-tubulin in a dose-dependent manner in SH-SY5Y cells[1].
HDAC-IN-94 (10 nM-30 μM, 24-72 h) shows no cytotoxicity in HEK-293 cells at concentrations up to 30 μM[1].
HDAC-IN-94 (24-72 h) shows antiproliferation activity against U87-MG, T98G, U251-MG and SH-SY5Y cells, with IC50s of 51.31, 42.60, 2.37, and 3.32 μM, respectively[1].
HDAC-IN-94 (3 μM, 24 h) promotes G2/M cell cycle arrest, triggers programmed cell death, and induces a minor autophagy stimulation in SH-SY5Y cells[1].
HDAC-IN-94 (3-30 μM, 24-72 h) demonstrates a clear time- and concentration-dependent pro-apoptotic activity in SH-SY5Y cells[1].

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

HDAC-IN-94 Related Antibodies

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 1 and 10 μM
Incubation Time: 24 h
Result: Promoted acetylation of α-tubulin in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Led to an accumulation of hypodiploid SH-SY5Y cells in the subG0/G1 phase.
Showed a decrease in the G0/G1 population and a slight increase in cells within the S-phase.

Apoptosis Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 3, 10, and 30 μM
Incubation Time: 24, 48 and 72 h
Result: Induced a concentration-dependent increase in early apoptosis at 24 h.
Induced a significant increase of late apoptosis starting at 10 μM (24 h).
Showed significant effects on both early and late apoptosis at 10 μM and a pronounced apoptotic response at 30 μM (46 % for early and 27 % for late apoptosis), at 48 h of treatment.
Significantly increased early and late apoptosis at all concentrations at 72 h.
Induced a concentration-dependent increase in caspase-3/7 activation, starting from 10 μM at 24 h.
Elicited 24% caspase-positive cells at 30 μM at 24 h.
Showed a significant increase in caspase activation at 10 μM and 30 μM at 48 h.
Continued to activate caspase-3/7 in a concentration-dependent manner after 72 h, with 43 % positivity at 30 μM.
Molecular Weight

342.35

Formula

C18H18N2O5
SMILES

O=C(NCC1=CC=C(C(NO)=O)C=C1)/C=C/C2=CC(OC)=C(O)C=C2
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-94 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-94HDACMicrotubule/TubulinApoptosisCaspaseHistone deacetylasesHDAC6α-tubulinneuroblastomaglioblastomaU87-MGT98GU251-MGSH-SY5YInhibitorinhibitorinhibit

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