Chromatin/Epigenetics

Epigenetics
Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.
Products for Chromatin/Epigenetics
- Bromodomain(43)
- Aurora Kinase(55)
- DNA Methyltransferase(30)
- HDAC(167)
- Histone Acetyltransferases(60)
- Histone Demethylases(83)
- Histone Methyltransferase(184)
- HIF(83)
- JAK(132)
- MBT Domains(1)
- PARP(93)
- Pim(27)
- Protein Ser/Thr Phosphatases(31)
- RNA Polymerase(6)
- Sirtuin(62)
- Sphingosine Kinase-2(1)
- Polycomb repressive complex(2)
- SUMOylation(3)
- PAD(16)
- Epigenetic Reader Domain(186)
- MicroRNA(12)
- Protein Arginine Deiminase(11)
- Chromodomain(1)
- Citrullination(15)
- DNA/RNA Demethylation(1)
- DNA/RNA Methylation(6)
- Histone Deacetylation(37)
- Histones/Histone Peptides(7)
- Tandem Tudor & Tudor-like Domains(1)
- Cat.No. Product Name Information
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GC68474
Pivanex
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GC68439
GNE-064
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GC68405
Lys-CoA TFA
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GC68378
GDC-4379
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GC68161
5-AIQ
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GC68147
dAURK-4 hydrochloride
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GC68035
PARP10/15-IN-1
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GC68025
UNC1021
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GC68010
HDAC3-IN-T247
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GC68006
PARP1-IN-11
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GC68000
JAK-IN-23
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GC67984
Alteminostat
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GC67962
Simmiparib
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GC67941
HIF-PHD-IN-1
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GC67934
EEDi-5285
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GC67921
Bomedemstat ditosylate
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GC67912
Amredobresib
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GC67906
OM-153
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GC67899
Aurora kinase inhibitor-8
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GC67873
PAD-IN-2
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GC67867
VVD-118313
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GC67863
DDO-2093 dihydrochloride
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GC67778
Sirtuin modulator 3
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GC67758
MM-401 TFA
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GC67676
Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
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GC67674
CRA-026440 hydrochloride
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GC52479
Histone H3 (Citrullinated R26) (21-44)-GGK-biotin Peptide (trifluoroacetate salt)
A biotinylated peptide fragment of histone H3
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GC52371
Vimentin (G146R) (139-159)-biotin Peptide
A biotinylated mutant vimentin peptide
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GC52370
Citrullinated Vimentin (R144) (139-159)-biotin Peptide
A biotinylated and citrullinated vimentin peptide
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GC52368
DL-Sulforaphane Glutathione
A metabolite of sulforaphane
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GC52367
Citrullinated Vimentin (G146R) (R144 + R146) (139-159)-biotin Peptide
A biotinylated and citrullinated mutant vimentin peptide
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GC52364
Vimentin (139-159)-biotin Peptide
A biotinylated vimentin peptide
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GC52363
Citrullinated Histone H3 (R2 + R8 + R17) (2-22)-biotin Peptide
A biotinylated and citrullinated histone H3 peptide
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GC52351
Citrullinated α-Enolase (R8 + R14) (1-19)-biotin Peptide
A biotinylated and citrullinated α-enolase peptide
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GC66464
HIF-1α-IN-2
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
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GC66441
BRD4/CK2-IN-1
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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GC66379
AFM-30a hydrochloride
AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a hydrochloride can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis.
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GC66335
PAD2-IN-1 hydrochloride
PAD2-IN-1 hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).
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GC66329
NDI-034858
NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.
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GC66067
ODM-207
ODM-207 (BET-IN-4) is a potent BET bromodomain protein (BRD4) inhibitor, with an IC50 of ≤ 1 μM.
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GC66055
5-Phenylpentan-2-one
5-Phenylpentan-2-one is a potent histone deacetylases (HDACs) inhibitor. 5-Phenylpentan-2-one can be used for urea cycle disorder research.
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GC66052
HDAC-IN-40
HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with Ki values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects.
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GC66049
NSC 694621
NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 μM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells.
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GC66026
SIRT2-IN-9
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer.
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GC65980
EZH2-IN-13
EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.
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GC65965
MPT0E028
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
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GC65962
Dot1L-IN-5
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
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GC65927
PARP-2-IN-1
PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
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GC65918
AS-85
AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78μM.
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GC65907
KSQ-4279
KSQ-4279 (USP1-IN-1, Formula I) is a USP1 and PARP inhibitor (extracted from patent WO2021163530).
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GC65899
AZ3391
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).
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GC65879
Bomedemstat hydrochloride
Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
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GC52188
MDL 800
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GC52166
NN-390
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
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GC65602
CFT8634
CFT8634 is a degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors.
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GC65581
MIND4-19
MIND4-19 is a potent SIRT2 inhibitor with an IC50 value of 7.0 μM.
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GC65574
SNIPER(BRD)-1
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively.
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GC65570
HIF1-IN-3
HIF1-IN-3 (compound F4) is a potent HIF1 inhibitor with an EC50 value of 0.9 μM. HIF1-IN-3 can be used for researching anticancer.
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GC65569
BRD4 Inhibitor-24
BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A).
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GC65546
DNMT3A-IN-1
DNMT3A-IN-1 is a potent and selective DNMT3A inhibitor.
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GC65509
PROTAC EZH2 Degrader-1
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.
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GC65506
BETd-246
BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
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GC65460
HDACs/mTOR Inhibitor 1
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
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GC65456
T-448
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM.
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GC65453
JAK-IN-3
JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
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GC65426
CM-675
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively.
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GC65405
JAK2-IN-6
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
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GC65387
Tyk2-IN-5
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα.
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GC65333
PT2399
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
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GC65330
AES-135
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM.
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GC65326
GNE-375
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin.
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GC65289
Lademirsen
Lademirsen (SAR339375; RG-012) is a single stranded, chemically modified oligonucleotide that binds to and inhibits the function of miR-21.
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GC65278
PIM1-IN-1
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
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GC65269
ZXH-3-26
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.
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GC65254
MC4355
MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC).
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GC65242
TFMB-(S)-2-HG
TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML).
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GC65206
FT895
FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
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GC65204
ZL0454
ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
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GC65202
Nesuparib
Nesuparib is a potent inhibitor of PARP.
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GC65201
Quercetagetin
Quercetagetin (6-Hydroxyquercetin) is a flavonoid.
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GC65186
DC-S239
DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.
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GC65160
FHT-1015
FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67).
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GC65147
PROTAC PARP1 degrader
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
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GC65138
NCDM-32B
NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
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GC65135
VZ185
VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
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GC65133
(S,R,S)-AHPC-C5-COOH
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized?E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
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GC65046
M1002
M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors.
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GC65045
(S)-MRTX-1719
(S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM.
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GC65037
MM-589 TFA
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
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GC65030
Sirtuin modulator 2
Sirtuin modulator 2 (Compound 132) is a sirtuin modulator with an ED50 equal or less than 50 μM.
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GC65027
PRMT5-IN-20
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity.
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GC65019
SRT 1460
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
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GC64999
MS402
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively.
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GC64968
SW-100
SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes.
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GC64960
BRD4 Inhibitor-10
BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM.
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GC64959
JAK/HDAC-IN-1
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
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GC64946
SRT 2183
SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
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GC64945
M1001
M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.
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GC64942
CHDI-390576
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
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GC64941
PR5-LL-CM01
PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.