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 ǰȳ  Ű   Pharmacology

Epigenetics Small Molecules

Epigenetics ʿ small molecule ȳ帳ϴ.

TOCRIS
ǰ ϱ
μϱ




Inhibitors
Cat. No. Product Name / Activity
4946 AIM 100
Potent and selective Ack1 (TNK2) inhibitor
5310 ASP 3026
Potent Ack (TNK2) inhibitor; also inhibits anaplastic lymphoma kinase (ALK)
5607 GNF 7
Ack1 and GCK inhibitor; inhibits Ras signaling
5098 KRCA 0008
Potent Ack1 and ALK dual inhibitor; orally bioavailable
6061 XMD 8-87
Potent Ack1/TNK2 inhibitor



Inhibitors
Cat. No. Product Name / Activity
5970 BAY 299
Potent and selective BRD1 and TAF1 inhibitor
5266 BAZ2-ICR
Selective BAZ2 inhibitor
5590 BI 9564
Potent and selective BRD9 and BRD7 inhibitor; orally active
4758 Bromosporine
Broad spectrum bromodomain inhibitor
5331 CPI 203
BET bromodomain inhibitor; arrests cell cycle at G1 phase
5635 GSK 2801
Selective BAZ2A and BAZ2B inhibitor
5385 GSK 5959
Potent and selective BRPF1 inhibitor
6198 GSK 6853
Potent and selective BRPF1 inhibitor
4650 I-BET 151 dihydrochloride
BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
6521 I-BET 762
Potent and high affinity BRD inhibitor; anti-inflammatory; orally bioavailable.
5591 I-BRD9
Potent and selective BRD9 inhibitor
4891 I-CBP 112
Selective CBP/p300 BRD inhibitor
4695 Ischemin sodium salt
CBP inhibitor; cell permeable
5806 ISOX DUAL
Dual BRD4 and CBP/p300 bromodomain inhibitor
4499 (+)-JQ1
Potent and selective BET bromodomain inhibitor; cell permeable
6251 L Moses dihydrochloride
High affinity and selective PCAF bromodomain inhibitor
6068 Lin28 1632
Bromodomain inhibitor; also RNA binding protein Lin28 inhibitor and promotes mESC differentiation
5496 LP 99
Selective BRD7 and BRD9 inhibitor
2418 LY 303511
BRD2, BRD3 and BRD4 inhibitor; also negative control of LY 294002
5173 MS 436
Potent and selective BRD4(1) inhibitor
5786 NI 42
High affinity BRPF inhibitor
5546 NI 57
Potent and selective BRPF bromodomain inhibitor
5744 NVS-CECR2-1
Potent and selective inhibitor of cat eye syndrome chromosome region, candidate 2 (CECR2)
5289 OF 1
Selective BRPF1B and BRPF2 inhibitor
6181 OTX 015
BET bromodomain inhibitor; orally bioavailable
4928 OXF BD 02
Selective BRD4(1) inhibitor
5801 PF CBP1
Selective CBP/p300 bromodomain inhibitor
4445 PFI 1
BET bromodomain inhibitor
5072 PFI 3
Potent and selective SMARCA2/4 and polybromo 1 inhibitor
5576 PFI 4
Potent and selective BRPF1B bromodomain inhibitor
4889 SGC-CBP30
Potent CBP/p300 BRD inhibitor
6000 TP 472
Potent BRD9/7 inhibitor
4132 XMD 8-92
BRD4 inhibitor; also ERK5/BMK1 inhibitor
Controls
Cat. No. Product Name / Activity
6155 cis MZ 1
Negative Control for MZ 1 (Cat. No. 6154)
5497 ent-LP 99
Negative Control for LP 99
6203 GSK 9311 hydrochloride
Negative control for GSK 6853
5808 ISOX INACT
Negative control for PF-CBP1
5603 (-)-JQ1
Inactive control for (+)-JQ1
5999 TP 472N
Negative control for TP 472
Others
Cat. No. Product Name / Activity
6356 AT 1
(+)-JQ1 based PROTAC with selectivity for BRD4
6327 dBET1
(+)-JQ1 based PROTAC targeting BET bromodomains, active in vivo
6588 (+)-JQ1 carboxylic acid
Carboxylic acid-functionalized BET bromodomain inhibitor
6589 (+)-JQ1 PA
Functionalized BET bromodomain inhibitor; 'click' ligand for PROTACs
6154 MZ 1
(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
6105 TC AC 28
High affinity BET bromodomain ligand
6936 VZ 185
Potent and selective BRD7/9 Degrader
6713 ZXH 3-26
Potent and selective BRD4 degrader


Inhibitors
Cat. No. Product Name / Activity
6284 BRD 73954
Dual histone deacetylase (HDAC) 6/8 inhibitor
2952 CI 994
Class I histone deacetylase inhibitor; orally active
3515 FK 228
Potent and selective class I histone deacetylase inhibitor; antitumor
5727 MC 1742
Potent class I and IIb HDAC inhibitor
5647 MI 192
Potent and selective HDAC2/3 inhibitor
6208 MS 275
HDAC (Class I) inhibitor
4902 NSC 405020
Histone deacetylase inhibitor
4643 PCI 34051
Potent and selective HDAC8 inhibitor
4403 Pyroxamide
Histone deacetylase inhibitor
6728 RGFP 966
Potent and selective HDAC3 inhibitor
3810 SBHA
HDAC1/3 inhibitor
4270 TC-H 106
Class I histone deacetylase inhibitor
5588 UF 010
Class I HDAC inhibitor


Inhibitors
Cat. No. Product Name / Activity
6010 BRD 4354
HDAC5 and HDAC9 inhibitor
6284 BRD 73954
Dual histone deacetylase (HDAC) 6/8 inhibitor
6040 BRD 9757
Potent and selective HDAC6 inhibitor
6725 CHDI 00390576
Potent and selective class IIa HDAC inhibitor; brain penetrant
4830 LMK 235
Selective HDAC4/HDAC5 inhibitor
4077 MC 1568
Selective HDAC class IIa inhibitor
5727 MC 1742
Potent class I and IIb HDAC inhibitor
7051 Tasquinimod
High affinity HDAC4 negative allosteric modulator; also binds S100A9; antiangiogenic
4805 TCS HDAC6 20b
Selective HDAC6 inhibitor
3402 Tubacin
HDAC6 inhibitor; inhibits a-tubulin deacetylation
6270 Tubastatin A hydrochloride
Potent HDAC6 inhibitor


Inhibitors
Cat. No. Product Name / Activity
3233 AGK 2
Selective SIRT2 inhibitor
4754 AK 7
Selective SIRT2 inhibitor; brain penetrant
2780 EX 527
Selective SIRT1 inhibitor
4127 Salermide
SIRT1 and SIRT2 inhibitor
5457 SirReal 2
Selective inhibitor of SIRT2
3521 Sirtinol
Selective sirtuin family deacetylase inhibitor
1542 Splitomicin
Sir2p inhibitor
Activators
Cat. No. Product Name / Activity
4590 Honokiol
SIRT3 activator; also blocks NF-κB activation
1418 Resveratrol
SIRT1 activator
5667 YK 3-237
SIRT1 activator



Inhibitors
Cat. No. Product Name / Activity
3842 5-Azacytidine
DNA methyltransferase inhibitor
2624 Decitabine
DNA methyltransferase inhibitor
4524 EGCG
DNMT1 inhibitor
5016 Fisetin
DNMT1 inhibitor
4359 Lomeguatrib
MGMT inhibitor
3295 RG 108
Non-nucleoside DNA methyltransferase inhibitor
5155 SGI 1027
DNA methyltransferase inhibitor
2293 Zebularine
DNA methyltransferase and cytidine deaminase inhibitor
Others
Cat. No. Product Name / Activity
1745 5-Iodotubercidin
Potent adenosine kinase inhibitor; decreases DNA methylation
6615 KCC 07
MBD2 (Methyl-CpG-binding domain protein 2) inhibitor
4061 6-Thioguanine
Anticancer and immunosuppressive agent; disrupts cytosine methylation


Inhibitors
Cat. No. Product Name / Activity
6384 Ciclopirox
Pan-histone demethylase inhibitor
4684 Daminozide
Selective KDM2/7 inhibitor
4593 GSK J1
Potent JMJD3/UTX inhibitor
4688 GSK J2
Inactive isomer of GSK J1 (Cat. No. 4593)
4594 GSK J4
Histone KDM inhibitor; cell permeable
5361 GSK LSD 1 dihydrochloride
Potent and selective LSD1 inhibitor
6124 (R)-2-Hydroxyglutaric acid disodium salt
KDM4A inhibitor; also NF-κB activator
4464 IOX 1
Histone demethylase inhibitor; cell permeable
4972 JIB 04
Pan Jumonji inhibitor; active in vivo
5287 NSC 636819
KDM4A/KDM4B inhibitor
6244 OG-L002
Potent LSD1 inhibitor
5930 PBIT
JARID1 (Jumonji AT-Rich Interactive Domain 1) inhibitor
4977 RN 1 dihydrochloride
LSD1 inhibitor
5714 S 2101
LSD1 inhibitor
5089 TC-E 5002
Selective KDM2/7 inhibitor
3852 Tranylcypromine hydrochloride
Irreversible inhibitor of LSD1; also inhibits MAO
Others
Cat. No. Product Name / Activity
6935 GSK J5 HCl
Inactive isomer of GSK J4 (Cat. No. 4594); cell permeable



Inhibitors
Cat. No. Product Name / Activity
4703 3-Deazaneplanocin A hydrochloride
EZH2 histone methyltransferase inhibitor
6790 GSK 126
Very high affinity and selective EZH2 inhibitor
6128 GSK 343
Potent and selective SAM-competitive EZH2 inhibitor
6153 JQEZ5
Potent and selective SAM-competitive EZH2 inhibitor
6169 PF 06726304 acetate
Highly potent and SAM-competitive EZH2 inhibitor
6708 SAH-EZH2
EZH2/EDD interaction inhibitor; suppresses PCR2 complex function
4904 UNC 1999
Potent and selective EZH2/EZH1 inhibitor
4930 UNC 2399
Biotinylated UNC 1999 (Cat.No. 4904)
5847 ZLD 1039
Potent and selective EZH2 inhibitor; orally bioavailable
Controls
Cat. No. Product Name / Activity
4905 UNC 2400
Negative control of UNC 1999 (Cat. No. 4904)



Inhibitors
Cat. No. Product Name / Activity
5163 A 366
Potent and selective G9a/GLP inhibitor
3364 BIX 01294
GLP and G9a inhibitor
6282 BRD 4770
G9a inhibitor and S-adenosyl methionine mimetic; cell permeable
3861 UNC 0224
Potent G9a and GLP inhibitor
4343 UNC 0638
Selective G9a and GLP inhibitor
5132 UNC 0642
Potent and selective G9a and GLP inhibitor
4342 UNC 0646
Potent and selective G9a and GLP inhibitor



Inhibitors
Cat. No. Product Name / Activity
6387 A 485
Potent and selective p300/CBP inhibitor; orally bioavailable
3084 Anacardic acid
Noncompetitive PCAF/p300 inhibitor
4200 C 646
Selective p300/CBP inhibitor
5646 EML 425
Reversible and non-competitive CBP/p300 inhibitor
5806 ISOX DUAL
Dual CBP/p300 and BRD4 bromodomain inhibitor
5045 L002
p300 inhibitor
5103 Lys-CoA
Selective p300 inhibitor
4903 NU 9056
Inhibitor of KAT5 (Tip60)
5964 SI-2 hydrochloride
Steroid receptor coactivator 3 (SRC-3) inhibitor
6692 WM 1119
High affinity KAT6A (MOZ) competitive inhibitor
Others
Cat. No. Product Name / Activity
4891 I-CBP 112
Selective CBP/p300 BRD inhibitor
4889 SGC-CBP30
Potent CBP/p300 BRD inhibitor


Inhibitors
Cat. No. Product Name / Activity
4666 UNC 1215
Potent inhibitor of L3MBTL3 Kme reader domain; cell permeable
4516 UNC 926 hydrochloride
L3MBTL1 domain inhibitor



Inhibitors
Cat. No. Product Name / Activity
4846 Apicidin
Potent histone deacetylase inhibitor
6249 Givinostat hydrochloride
Histone deacetylase inhibitor
2771 M 344
Histone deacetylase inhibitor
3747 NCH 51
Histone deacetylase inhibitor
2521 NSC 3852
Histone deacetylase inhibitor
2682 Sodium 4-Phenylbutyrate
Histone deacetylase inhibitor
4652 SAHA
Class I and II HDAC inhibitor
2421 Scriptaid
Histone deacetylase inhibitor
3850 Sodium butyrate
Histone deacetylase inhibitor
1406 Trichostatin A
Potent histone deacetylase inhibitor
2815 Valproic acid, sodium salt
Histone deacetylase inhibitor


Inhibitors
Cat. No. Product Name / Activity
5128 C 21
Selective PRMT1 inhibitor
6516 EPZ 015666
Potent and selective PRMT5 inhibitor
5202 Furamidine dihydrochloride
Selective PRMT1 inhibitor
5777 GSK 591 dihydrochloride
Potent and selective PRMT5 inhibitor
5713 MS 023 dihydrochloride
Potent and selective type I PRMT inhibitor
5685 MS049 oxalate salt
Potent and selective PRMT4 and PRMT6 inhibitor
5367 SGC 707
Potent and selective allosteric inhibitor of PRMT3
5099 TC-E 5003
Selective PRMT1 inhibitor
6008 TP 064
Potent and selective PRMT 4 inhibitor
5057 UNC 2327
Allosteric inhibitor of PRMT3
Controls
Cat. No. Product Name / Activity
5450 XY1
Negative control of SGC 707 (Cat. No. 5367)


Inhibitors
Cat. No. Product Name / Activity
5307 MM 102
Potent WDR5/MLL interaction inhibitor
5267 OICR 9429
High affinity and selective WDR5 antagonist
5323 WDR5 0103
WDR5 antagonist