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Cat. No.: HY-170379

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HDAC-IN-84

HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC₅₀ values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity.

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화학식: C₁₇H₂₁N₃O₅S
분자량:379.43

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

HDAC-IN-84 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

HDAC1

0.0045 μM (IC₅₀)

HDAC2

0.015 μM (IC₅₀)

HDAC-3

0.013 μM (IC₅₀)

HDAC4

>100 μM (IC₅₀)

HDAC6

0.038 μM (IC₅₀)

HDAC8

5.8 μM (IC₅₀)

HDAC11

26 μM (IC₅₀)

All HDAC Isoforms :

In Vitro

HDAC-IN-84 (95min) inhibits HDAC1, HDAC2, HDAC3, HDAC4, HDAC6, HDAC8 and HDAC11 with IC₅₀ values of 0.0045, 0.015, 0.013, >100, 0.038, 5.8 and 26 μM, respectively^[1].
HDAC-IN-84 (0.005-25 μM, 72 h) inhibits HL60, HPBALL, and K562 cells with IC₅₀s of 76.8, 110.6 and 180.8 nM respectively^[1].
HDAC-IN-84 (0.25 μM, 48 h) results in notable α-tubulin acetylation and higher PARP cleavage of HDAC6^[1].
HDAC-IN-84 (0.25 μM, 48 h) induces Apoptosis in HL60 cells^[1].
HDAC-IN-84 (0.15-0.2 μM, 24 h) induces cell cycle arrest in HL60 cells^[1].
HDAC-IN-84 (2.5, 50 nM, 1 μM, 24 h) demonstrates excellent stability over the 24 h period monitored in human plasma at 37 °C^[1].
HDAC-IN-84 (2.5, 50 nM, 1 μM, 48 h) binds with plasma protein with a mean of 99.0% over the observed concentration range with no concentration-dependency^[1].
HDAC-IN-84 (0-1 μM) inhibits MV4-11 cells with an IC₅₀ of 0.036 μM, exhibiting over a 7-fold increase inpotency compared to Vorinostat (HY-10221) ^[1].
HDAC-IN-84 (0-10 μM, 72 h) and Vorinosta (HY-10221) affects C1498 cell growth in a concentration-dependent manner with IC₅₀s of 0.425 and 1.06 μM, respectively^[1].
Comparison of In Vitro Pharmacokinetic Data of HDAC-IN-84 to Vorinostatas

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

Apoptosis Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.25 μM
Incubation Time:

48 h
Result:

Induced Apoptosis, leading to cytotoxic impacts on leukemia cells.

Cell Viability Assay^[1]

Cell Line:

K562, HL60, HPBALL cells
Concentration:

0.005-25 μM
Incubation Time:

72 h
Result:

Inhibited HL60, HPBALL, and K562 cells with IC₅₀s of 76.8, 110.6 and 180.8 nM respectively.

Western Blot Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.25μM
Incubation Time:

48 h
Result:

Resulted in notable α-tubulin acetylation (indicating effective inhibition) of HDAC6.
Resulted in higher PARP cleavage (indicator of apoptosis induction).

Cell Cycle Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.15, 0.2 μM
Incubation Time:

24 h
Result:

Induced cell cycle arrest in leukemia cells.

In Vivo

HDAC-IN-84 (10 mg/kg, i.p., daily, 14 days) suppresses MV4-11 and C1498 cells growth in a preclinical leukemic xenograft mouse (NSG) model^[1].
HDAC-IN-84 (10 mg/kg, i.p.) is characterized by a short elimination half-life of 0.35 h in three C57BL/6 mice. ^[1].
HDAC-IN-84 (20 mg/kg, i.p., daily, 21 days) exhibits significantly lower leukemia burden, with no significant differences in body weight in allograft leukemia model^[1].
Pharmacokinetic Parameters (AUC_last, C_max, T_max, and t_1/2) Were Calculated According to a Noncompartmental Analysis (NCA) from the Blood Concentration of HDAC-IN-84 Based on Actual Blood Sampling Time Pre-Dose and Post-Dose

	vorinostatas	HDAC-IN-84
log D	1.46	1.47
plasma stability/t_1/2	75 min	>24 h
K_B/P	2.0	1.26
plasma protein binding	71%	99%
microsomal stability/t_1/2( clearance category)	60 min	35.9 min

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

Animal Model:

preclinical leukemic xenograft mouse (NSG) model. Each mouse received 0.5 × 10⁶ MV4-11 luc-GFP+ leukemic cells. After confirmation of tumor engraftment via monitoring bioluminescence-based in vivo imaging system (IVIS)^[1].

Significantly suppressed the in vivo growth of MV4-11 leukemia cells as compared to the vehicle control.
Exhibited a minor (not significant) reduction in body weight.

Animal Model:

Allograft leukemia model. In this model, leukemia is established by injecting (C57BL/6) derived murine AM L(C1498) cells by intravenous injection in immunocompetent wildtpye (C57BL/6) mice [1] .

Exhibited significantly lower leukemia burden after the second treatment cycle, with this difference becoming more pronounced by day 19.
No significant differences in body weight were observed during the treatment course.

Chemical Information

분자량 379.43
화학식 C₁₇H₂₁N₃O₅S
SMILES

O=C(C1=NC(C2=CC=C(OC)C=C2)=CS1)NOCCCCCC(NO)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Fischer F, et.al. Deciphering the Therapeutic Potential of Novel Pentyloxyamide-Based Class I, IIb HDAC Inhibitors against Therapy-Resistant Leukemia. J Med Chem. 2024 Dec 12;67(23):21223-21250. [Content Brief]

Calculators

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Mass Mass

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Molecular Weight Molecular Weight

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

variable	mouse 1	mouse 2	mouse 3	mean [±SD]	Vorinostat	Vorinostat
		intraperitoneal 10 mg/kg			per oral 50 mg/kg
C_max (ng/mL)	1490	1030	1230	1250[±232]	501	580
T_max (h)	0.25	0.25	0.25	0.25[±0]	na	0.08
AUC_last (h・ng/mL)	523	396	480	466[±65]	619	347
t_1/2	0.275	0.554	0.227	0.352[±0.177]	0.75	0.8

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