2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. CZL-149

CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC50s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma.

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CZL-149

CZL-149 Chemical Structure

CAS No. : 3094772-96-7

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CZL-149 Related Antibodies

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Description

CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC50s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma[1].

IC50 & Target[1]

p300

10.5 nM (IC50, TSA Assay)

BRD4 BD1

13 nM (IC50, AlphaScreen Assay)

BRD4 BD2

78 nM (IC50, AlphaScreen Assay)

BRD4 BD1

2 nM (IC50, HTRF Assay)

BRD4 BD2

22 nM (IC50, HTRF Assay)

CBP

183 nM (IC50, AlphaScreen Assay)

p300

118 nM (IC50, AlphaScreen Assay)

In Vitro

Thermal displacement analysis (TSA) showed that CZL-149 (compound 14) inhibits the p300 bromine domain with an IC50 of 10.5 nM[1].
AlphaScreen analysis showed that CZL-149 exhibits strong inhibitory activity against BRD4 BD1 (IC50: 10 nM) and BRD4 BD2 (IC50: 80 nM)[1].
CZL-149 (6 days) shows antiproliferative activity against OPM-2 cells, with an IC50 value of 3.3 nM[1].
CZL-149 binds most strongly to BET family proteins (BRD2/3/4/T), followed by CECR2 and p300/CBP[1].
AlphaScreen results shows that CZL-149 inhibits BRD4 BD1 and BD2 with IC50 values ​​of 13 nM and 78 nM, respectively; and inhibits p300 and CBP bromodomain with IC50 values ​​of 118 nM and 183 nM, respectively. HTRF results showed that CZL-149 has a strong inhibitory effect on BRD4 BD1 and BD2, with IC50 values ​​of 2 nM and 22 nM, respectively[1].
In OPM-2 cells, CZL-149 (50 nM; 72 h) significantly downregulates the expression of AGAP7P, SLC3A2, VAT1, SLC1A5, LONP1, AARS1, GADD45A, VEGFA, SESN2 and DBN1 genes[1].
In OPM-2 cells, CZL-149 (10-50 nM) inhibits c-Myc and H3K27Ac levels in a dose-dependent manner[1].
CZL-149 exhibits high microsomal stability in mouse, rat and human liver microsomes, with half-lives of 145 minutes (mouse), 205 minutes (rat) and 118 minutes (human), respectively[1].

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

CZL-149 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t F CL Vss
Mice[1] 10 mg/kg p.o. 0.98 h 2081 ng/mL 3086 ng·h/mL 107 % / /
Mice[1] 2 mg/kg i.v. 0.72 h / 577 ng·h/mL / 57.1 mL/min/kg 2.5 L/kg
In Vivo

CZL-149 (10 mg/kg; p.o.; once daily; for 21 days) has antitumor efficacy in OPM-2 mouse xenograft model[1].
CZL-149 (10 mg/kg; p.o.; once daily; for 7 days) displays an improved safety profile in C57BL/6 mice[1].
CZL-149 (20 mg/kg; oral; single dose) accumulates primarily in the liver in mice, with low levels detected in the heart and brain[1].

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

Animal Model: Nude mice were injected subcutaneously with 5 × 106 OPM-2 cells[1].
Dosage: 10 mg/kg
Administration: p.o.; once daily; for 21 days
Result: Significantly suppressed tumor growth, achieving a tumor growth inhibition (TGI) of 78%.
Showed better tolerated in mice.
Animal Model: Female C57BL/6 mice (6-8 weeks)[1].
Dosage: 10 mg/kg
Administration: p.o.; once daily; for 7 days
Result: Did not cause a significant reduction in platelet count.
Showed good hematological safety.
Molecular Weight

460.45

Formula

C23H23F3N4O3
CAS No.
SMILES

O=C1C2=C(C(C3=CC4=C(N=C(C5CCOCC5)N4CCOC(F)(F)F)C=C3)=CN1C)C=CN2
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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CZL-149 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:

CZL-1493094772-96-7CZL149CZL 149Epigenetic Reader DomainHistone AcetyltransferaseHATsHATBET inhibitorp300/CBP bromodomains inhibitorBED4 BD1BED4 BD2c-MycH3K27Acmultiple myelomadrug-like propertiesInhibitorinhibitorinhibit

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