1. Epigenetics Cell Cycle/DNA Damage
  2. Epigenetic Reader Domain HDAC
  3. TW9

TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026).

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TW9 Chemical Structure

TW9 Chemical Structure

CAS No. : 2614417-90-0

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Description

TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026)[1].

IC50 & Target[1]

BRD4(1)

0.069 μM (Kd)

BRD4(2)

0.231 μM (Kd)

HDAC1

0.29 μM (IC50)

Molecular Weight

610.13

Formula

C32H28ClN7O2S

CAS No.
SMILES

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(NC4=CC=C(C=C4)C(NC5=C(C=CC=C5)N)=O)=O)C6=NN=C(C)N26

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Purity & Documentation
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  • 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.

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TW9
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HY-155222
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