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TCIP 1

Catalog No. T79801

TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

TCIP 1, CAS N/A

Pack Size	Availability	Price/USD
25 mg	Inquiry	$ 2,420.00
50 mg	Inquiry	$ 3,180.00
100 mg	Inquiry	$ 4,300.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].
In vitro	TCIP 1 enhanced the binding of BRD4 to BCL6 loci on the genome by 50%, while only reducing its binding at enhancers by 10%. This led to transcriptional elongation at pro-apoptotic target genes, significantly inhibiting diffuse large B-cell lymphoma cell lines, including chemotherapy-resistant TP53 mutant cell lines, with an EC50 of 1-10 nM [1]. The apoptosis induced by TCIP 1 could be blocked by either JQ1 (a BRD4 inhibitor) or BI3812 (a BCL6 inhibitor). TCIP 1 induced G1/S and G2/M cell cycle arrest in KARPAS422 cells. Further, TCIP 1 (10 or 100 nM; 20 h) significantly activated anti-apoptotic genes, while a 10 nM concentration for 8 h suppressed the expression of MYC and its target genes.
In vivo	TCIP1, administered intraperitoneally at a dosage of 10 mg/kg daily for five consecutive days, was well tolerated in wild-type C57BL/6 mice with a half-life (t 1/2) of 9.7 hours, a maximum concentration (C max) of 0.41 μM, and an area under the curve (AUC 0-last) of 1.92 μM/h [1].

Molecular Weight	1026.04
Formula	C50H58Cl2N12O6S

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Gourisankar S, Krokhotin A, Ji W, et al. Rewiring cancer drivers to activate apoptosis. Nature. 2023;620(7973):417-425.

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BET bromodomain inhibitor BAY-850 BRM/BRG1 ATP Inhibitor-1 TPOP146 Piflufolastat A-485 CBP/p300-IN-5 dBRD9 HCl

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TCIP 1 Chromatin/Epigenetic Epigenetic Reader Domain inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.