Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
21 Results for "
CoREST
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "CoREST" in MCE Product Catalog:
TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors .
Cat. No.: HY-172762
Target:
Research Areas:
S234984 is a molecular glue degrader. S234984 forms a stable ternary complex with wild-type KBTBD4 E3 ligase and HDAC2 to drive neomorphic ubiquitination and degradation of CoREST1 and LSD1. S234984 can be used for the research of medulloblastoma .
Cat. No.: HY-176875
Target:
Research Areas:
CoREST/LSD1 degrader-1 (Compound 4) is a molecular glue degrader targeting the KBTBD4 E3 ubiquitin ligase. CoREST/LSD1 degrader-1 is promising for research of KBTBD4-mutant driven cancers (e.g., medulloblastoma) and epigenetic dysregulation disorders .
(S)-TNG260 is an isomer of TNG260 (HY-153358). TNG260 is a CoREST selective deacetylase (CoreDAC) inhibitor. TNG260 inhibits HDAC1 with 10-fold selectivity over HDAC3. TNG260 causes HDAC1 inhibition and reverses anti-PD1 resistance driven by STK11 deletion. TNG260 reduces intratumoral infiltration of neutrophils. TNG260 exhibits immune-mediated cell killing.
Cat. No.: HY-176866
CAS No.: 2222756-46-7
Target:
Research Areas:
Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
Cat. No.: HY-175184
Target:
Research Areas:
LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC50 of 0.02 μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research .
Cat. No.: HY-176868
CAS No.: 2065162-16-3
Target:
Research Areas:
Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18 and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research .
Cat. No.: HY-176867
Target:
Research Areas:
Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
Cat. No.: HY-161849
Target:
Research Areas:
LSD1-IN-31 (compound 11e) can directly bind to LSD1/CoREST complex to reduce LSD1 demethylation enzymatic activity. LSD1-IN-31 inhibits LSD1 demethylation activity and influences its downstream IκB/NF-κB signaling pathway. LSD1-IN-31 inhibits osteoclastic bone loss in vitro and in vivo. LSD1-IN-31 can be used for osteoporosis research .
Cat. No.: HY-RS11791
Target:
Research Areas:
RCOR1 Human Pre-designed siRNA Set A contains three designed siRNAs for RCOR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-161848
Target:
Research Areas:
TCP-MP-CA (compound 11a) is an inhibitor of LSD1 demethylation enzymatic via binding to LSD1/CoREST complex. TCP-MP-CA exhibits an inhibitory effect on osteoclastogenesis, with an IC50 value of 0.14 µM .
Cat. No.: HY-175185
Target:
Research Areas:
MC3935 is a LSD1 inhibitor with an IC50 of 0.52 μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research .
Cat. No.: HY-144756
CAS No.: 3033060-62-4
Target:
Research Areas:
LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 9.9 μM .
Cat. No.: HY-144757
CAS No.: 3033060-68-0
Target:
Research Areas:
LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM .
Cat. No.: HY-144758
CAS No.: 3033060-70-4
Target:
Research Areas:
LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 17.2 μM .
Cat. No.: HY-183202
CAS No.: 1456907-39-3
Target:
Research Areas:
NCD38 is a Lysine-specific demethylase 1 (LSD1) inhibitor with a target IC50 of 0.59 μM. NCD38 selectively disrupts LSD1-GFI1B interactions, dissociates LSD1 and CoREST from the ERG super-enhancer. NCD38 increases apoptosis-related protein levels, induces apoptosis and reduces SOX2 and Oct4 levels. NCD38 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-182891
Target:
Research Areas:
MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC50 values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-RS22773
Target:
Research Areas:
Rcor2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rcor2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-182892
Research Areas:
MC4491 is a selective LSD1/PRMT5 inhibitor, with an IC50 of 0.152 μM against the LSD1/CoREST complex and an IC50 of 0.043 μM against the PRMT5/MEP50 complex. MC4491 induces transcriptomic changes and splicing alterations in AML cells. MC4491 is applicable for the research of acute myeloid leukemia .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
