2. PROTAC Epigenetics
  3. PROTACs Histone Acetyltransferase
  4. PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance.

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

PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 Chemical Structure

CAS No. : 3031606-85-3

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PROTAC KAT2A/B degrader-1 Related Antibodies

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Description

PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC KAT2A/B degrader-1 (Compound 24) induces potent degradation of KAT2A in MOLM-13 AML cells with a DC50 of 1.53 nM and 90% maximum degradation[1].
PROTAC KAT2A/B degrader-1 induces potent degradation of KAT2A (DC50 = 1.39 nM, Dmax = 95%) and KAT2B (DC50 16.5 nM) in NCI-H1048 SCLC cells[1].

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

PROTAC KAT2A/B degrader-1 Related Antibodies
Parmacokinetics
Species Dose Route CL T1/2 Vd F AUC Cmax
Mice[1] 1 mg/kg i.v. 1.0 mL/min/kg 5.3 h 0.4 L/kg / / /
Mice[1] 1 mg/kg p.o. / / / 47 % 101.3 nM·h 10.4 nM
In Vivo

PROTAC KAT2A/B degrader-1 (Compound 24) (1-50 mg/kg; p.o.; single dose) achieves and sustains free plasma concentrations above the H1048 KAT2A DC90 threshold (22 nM) for at least 24 hours at 50 mg/kg in CD-1 mice[1].

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

Animal Model: CD-1 mice[1]
Dosage: 1 mg/kg; 50 mg/kg
Administration: P.o.; single dose
Result: Reached a peak free plasma concentration of ~0.01 μM and remained above the H1048 KAT2A DC50 threshold (1.39 nM) through 8 hours, declining thereafter (1 mg/kg dose).
Reached a peak free plasma concentration of ~0.4 μM, remained above the H1048 KAT2A DC90 threshold (22 nM) for at least 24 hours, and demonstrated proportional increases in exposure relative to the 1 mg/kg dose (50 mg/kg dose).
Molecular Weight

619.07

Formula

C31H31ClN6O6
CAS No.
SMILES

CN1C[C@H](NC2=C(Cl)C(N(C)N=C2)=O)C[C@H](C3=CC=C(COC4=CC5=C(C(N(C6C(NC(CC6)=O)=O)C5=O)=O)C=C4)C=C3)C1
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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PROTAC KAT2A/B degrader-1 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:

PROTAC KAT2A/B degrader-13031606-85-3PROTACsHistone AcetyltransferaseHATsHATneuroendocrine prostate cancerMOLM-13 AML cellsNCI-H1048 SCLC cellsacute myeloid leukemiasmall cell lung cancerCD-1 miceKAT2BKAT2AInhibitorinhibitorinhibit

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