p300

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

CBP p300 ligand 2 is a selective ligand that binds to the target protein for PROTAC[dCBP-1], a potent and selective heterobifunctional degrader of p300 CBP.

CBP EP300-IN-2 is an inhibitor of CBP EP300 with IC50 values of 1.07 nM for CBP HTRF and 5.96 nM for Myc.

PROTAC CBP P300 Degrader-1 is an effective compound that potently degrades CBP P300, significantly reducing cell viability in various cancer cell lines.

CBP p300-IN-17 (compound 7) is a potent inhibitor of EP300 CBP HAT, with an IC50 of 0.18 μM for HAT EP300 and 0.69 μM for LK2 H3K27.

CBP p300-IN-19 hydrochloride is a selective and potent inhibitor of p300 CBP HAT, with IC50 values of 1.4 μM for p300-HAT, 2.2 μM for CBP-HAT, and over 100 μM for both PCAF and Myst3, and has antitumor effects.

P300 bromodomain-IN-1 is a potent inhibitor of p300 (EP300) bromodomain (IC50: 49 nM). p300 bromodomain-IN-1 blocks c-Myc expression and induces cell cycle arrest at G1/G0 phase and apoptosis in OPM-2 cells. apoptosis).

CBP/p300-IN-10, a potent inhibitor targeting histone acetyltransferase enzymes EP300 and CREBBP, exhibits IC50 values of 26 nM and 39 nM, respectively. This compound shows potential for anticancer research applications.

CBP p300-IN-15 (compound 13a) is a potent inhibitor of p300 (IC50: 2.5 nM) and CBP (IC50: 28.0 nM). It inhibits OVCAR-3 cells (EC50: 0.865 μM) and A2780 cells (EC50: 2.71 μM). CBP p300-IN-15 can be used to study ovarian cancer.

P300 CBP-IN-5 is a potent inhibitor of p300 CBP histone acetyltransferase (IC50 of 18.8 nM).

CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.

Thalidomide-NH-CBP p300 ligand 2 (P-007) is a PROTAC-based compound engineered to degrade the proteins CBP and p300, functioning as a molecular antagonist (WO2020173440).

CBP p300-IN-8 is a potent inhibitor of the CBP P300 family of bromodomains, inhibiting CBP with an IC50 range of 0.01-0.1 μM and BRD4 with an IC50 range of 1-1000 μM.

CBP p300-IN-18 (compound 8) is a potent inhibitor of EP300 CBP HAT, with an IC50 of 0.056 μM for HAT EP300 and 0.46 μM for LK2 H3K27.

CBP p300-IN-19 is a potent inhibitor of p300 CBP HAT, effective against P300-HAT (IC50: 1.4 μM), CBP-HAT (IC50: 1.4 μm, 2.2 μM), PCAF (IC50: >100 μM), and Myst3 (IC50: >100 μM), demonstrating anti-tumor activity.

CBP/p300-IN-14, efficiently inhibits CBP/EP300 (lysine acetyltransferase) with an IC50 value of 3.3 nM.

CBP p300-IN-16 (compound 1) is a potent inhibitor of EP300 CBP HAT, targeting HAT EP300 with an IC50 of 0.61 μM and LK2 H3K27 with an IC50 of 2.24 μM.

CBP p300-IN-21 (Compound 5d) is a selective inhibitor of CBP p300, with IC50 values of 0.07 μM for p300 and 1.755 μM for CBP; it reduces H3K18Ac levels and inhibits the growth of 4T1 tumors in mice [1].

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Diflunisal (Dolobid) is a cyclooxygenase (COX) Inhibitor, used as an anti-inflammatory analgesic.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

NEO2734 (EP31670) is an orally active, selective inhibitor of p300 CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.

iP300v is a negative control for iP300w

Ep300 CREBBP-IN-8 (Example 37), a potent and orally active inhibitor of Ep300 and CREBBP, shows IC50 values of 0.014 μM and 0.018 μM, respectively, and is utilized in cancer research [1].

Ep300 CREBBP-IN-3 (Example 61), a potent inhibitor of Ep300 and CREBBP with IC50 values of 0.056 μM and 0.095 μM, respectively, is applicable in cancer research [1].

Ep300 CREBBP-IN-2 (Example 73) is a potent, orally bioavailable inhibitor of Ep300 and CREBBP, with IC50 values of 0.052 μM and 0.148 μM, respectively, and is used in cancer research [1].

Ep300 CREBBP-IN-4 (Example 56), a potent inhibitor of both Ep300 and CREBBP, shows IC50 values of 0.024 μM and 0.064 μM, respectively, and is employed in cancer research [1].

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP p300 bromodomains.

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

dCBP-1 is a chemical degrader of p300 CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300 CBP. Degradation of p300 CBP by dCBP-1 leads to effective multiple myeloma cell killing.

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

UMB298 is a potent and selective CBP P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.

BRD32048 is the ETV1 transcription factor oncoprotein inhibitor.

L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.

IQ 1 has multiple roles, such as maintaining the multifunctionality of mouse ESCs, decreasing Wnt-stimulated phosphorylation, blocking PP2A/Nkd interactions, and so on.

C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

TTK21 is an activator of CBP p300 histone acetyltransferase activity.

Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.