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Cat. No.: HY-141429C

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AS-99

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 μM, K_d= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

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Formule: C₂₇H₃₁ClF₃N₅O₃S₂
Masse moléculaire:630.14

Stockage:

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

Data Sheet (276 KB)

AS-99 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

ASH1L/KMT2H

Voir tous les produits spécifiques à Isoform Histone Methyltransferase :

In Vitro

AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L^[1].
AS-99 shows a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, with no or limited effects at 10 μM or higher concentrations^[1].
AS-99 (1-8 μM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells^[1].
AS-99 suppresses MLL fusion driven transcriptional programs^[1].
AS-99 results in a reduced number of H3K36me2 peaks when compared to the DMSO-treated cells^[1].

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

RT-PCR^[1]

Cell Line:

MOLM13 cells
Concentration:

2-6 µM
Incubation Time:

7 days
Result:

Led to a dose-dependent downregulation of canonical MLL fusion target genes required for leukemogenesis including MEF2C, DLX2, FLT3, and HOXA9.

In Vivo

AS-99 (30 mg/kg; i.p.; q.d., treated for 14 consecutive days) reduces leukemia burden in mice^[1].
AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5-6 h) and C_max > 10 μM^[1].

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

Animal Model:

8- to 10-week old female NSG mice (bearing MV4;11 cells)^[1]
Dosage:

30 mg/kg
Administration:

I.p.; q.d., treated for 14 consecutive days
Result:

Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.

Chemical Information

Masse moléculaire 630.14
Formule C₂₇H₃₁ClF₃N₅O₃S₂
SMILES

O=C(C1CN(C)C1)NCC2=CC3=C(C=C2)C(C4=CC=CC(C(N)=S)=C4)=CN3C5CCN(S(=O)(C(F)(F)F)=O)CC5.[H]Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Publications (2)

All In Vivo Efficacy StudyIHCIn Vivo Imaging

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Nat Commun

Histone methyltransferase ASH1L primes metastases and metabolic reprogramming of macrophages in the bone niche. [Abstract]

2025 May 20;16(1):4681. PMID: 40394007

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

AS-99 (25 mg/kg, i.p.) treatment significantly suppressed metastases to bone and prolonged the overall survival of mice.

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

Multiplex IHC staining of TAMs in bone tumors treated with AS-99 (i.p., 25 mg/kg).

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

2 × 10⁶ PC-3M cells were intracardiac injected into male nude mice, followed by treatment of vehicle or ASH1L inhibitor AS-99 (i.p., 25 mg/kg). Bioluminescent imaging and intensity quantification of metastatic tumors on Day 34 are presented.
Adv Sci (Weinh)

ASH1L in Hepatoma Cells and Hepatic Stellate Cells Promotes Fibrosis-Associated Hepatocellular Carcinoma by Modulating Tumor-Associated Macrophages. [Abstract]

2024 Dec;11(45):e2404756. PMID: 39377228

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 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)
Instruction de manipulation (2659 KB)

Références

[1]. Rogawski DS, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14;12(1):2792. [Content Brief]

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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.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Pureté et documentation
Références

1/16
1/16

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

Customer Validation
AS-99 (25 mg/kg, i.p.) treatment significantly suppressed metastases to bone and prolonged the overall survival of mice.
1/16

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

Customer Validation
Multiplex IHC staining of TAMs in bone tumors treated with AS-99 (i.p., 25 mg/kg).
1/16

AS-99 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681. [Abstract]

Customer Validation
2 × 10⁶ PC-3M cells were intracardiac injected into male nude mice, followed by treatment of vehicle or ASH1L inhibitor AS-99 (i.p., 25 mg/kg). Bioluminescent imaging and intensity quantification of metastatic tumors on Day 34 are presented.

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AS-99

Publications Citing Use of MedChemExpress (MCE) AS-99

Voir tous les produits spécifiques à Isoform Histone Methyltransferase