| DC49037 |
1-Alaninechlamydocin |
1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells. |
|
| DC49107 |
BRD4-BD1/2-IN-2 |
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2). |
|
| DC49134 |
BRD4 D1-IN-1 |
BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC. |
|
| DC49150 |
BRD4 D1-IN-2 |
BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC. |
|
| DC49198 |
Biotinylated-JQ1 |
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for BRD4. |
|
| DC49199 |
UNC6212 (Kme2) |
UNC6212 (Kme2), a dimethyllysine (Kme2)-containing ligand, has a KD for CBX5 of 5.7 μM. |
|
| DC49234 |
UNC6349 (Ket2) |
UNC6349 (Ket2), a diethyllysine (Ket2)-containing ligand, binds to wild-type CBX5, with a KD of 3.2 μM. |
|
| DC49246 |
Bomedemstat ditosylate
Featured
|
Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity. |
|
| DC49247 |
UNC6864 (Kei) |
UNC6864 (Kei), an ethylisopropyllysine (Kei)-containing ligand, binds to wild-type CBX5, with a KD of 3.3 μM. |
|
| DC49269 |
OARV-771 |
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively. |
|
| DC49580 |
Cas9-IN-2 |
Cas9-IN-2 is a potent Cas9 inhibitor (IC50=246 μM), Cas9-IN-2 acts by binding to apo-Cas9 to prevent Cas9:gRNA complex formation, which can potentially be applied to modulate and control Cas9 activity in various applications. |
|
| DC49581 |
Cas9-IN-1 |
Cas9-IN-1 is a potent Cas9 inhibitor (IC50=7.02 μM), acting by binding to apo-Cas9 to prevent Cas9:gRNA complex formation. |
|
| DC49582 |
OKI-006 |
OKI-006 is a potent and orally active inhibitor of histone deacetylase (HDAC). OKI-006 is a unique congener of the natural product HDAC inhibitor largazole. Histone deacetylases (HDACs) play critical roles in epigenomic regulation, and histone acetylation is dysregulated in many human cancers. OKI-006 has the potential for the research of cancer disease. |
|
| DC49583 |
Elevenostat
Featured
|
Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235 µM). Anti-multiple myeloma (MM) activity. |
|
| DC49584 |
MPT0B390 |
MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM. |
|
| DC49585 |
MIR002 |
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo. |
|
| DC49586 |
PHD2/HDACs-IN-1 |
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI). |
|
| DC49587 |
CYD19
Featured
|
Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis. |
|
| DC49588 |
HDAC-IN-30 |
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy. |
|
| DC49589 |
KD 5170 |
KD 5170 is a pan inhibitor of histone deacetylases (HDACs) and exhibits broad spectrum antitumor activity in vitro and in vivo. |
|
| DC49590 |
MC4343 |
MC4343 is a potent and dual inhibitor of EZH2 and histone deacetylase. MC4343 has the potential for the research of cancer disease. |
|
| DC49591 |
NSC636819 |
NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer. |
|
| DC49592 |
LSD1-IN-14 |
LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells. |
|
| DC49593 |
AGK7 |
AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease. |
|
| DC49594 |
Sirt2-IN-5 |
Sirt2-IN-5 is a potent SIRT2 inhibtor. |
|
| DC49595 |
BRM/BRG1 ATP Inhibitor-2 |
BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders. |
|
| DC49596 |
FHT-1015 |
FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67). |
|
| DC49597 |
FHT-1204 |
FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70). |
|
| DC49598 |
(R,R)-CFT8634 |
(R,R)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,R)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 175). |
|
| DC49599 |
(R,S)-CFT8634 |
(R,S)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,S)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 176). |
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