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Chemical Probes
Chemical Probes
Potent, selective and cell-permeable inhibitors of protein function ("chemical probes") are valued reagents in both fundamental and applied biological research, and they are essential for the early stages of drug discovery by allowing preclinical target validation in both academic and industrial laboratories.
SGC chemical probes are open-access reagents that are meant to be used by the biomedical research community with no restrictions on use. To acquire a sample, follow the links on the webpage of your desired chemical probe. You can sort the table by clicking the column headers.
The SGC probes set is complemented by the donated probe set
Name | Structures | Protein family | Specific Targets | Control | In Vivo Activity* | Added |
---|---|---|---|---|---|---|
A-1596586 | Ion channel | CFTR | A-1596584 | No | 06/19 | |
GNE-2256 | Kinase | IRAK4 | GNE-6689 | Yes | 11/21 | |
A-366 | Methyltransferase | EHMT1/GLP, EHMT2/G9a | No | 06/13 | ||
BTZO-1 | Cytokine | MIF | BTZO-4 | No | 05/18 | |
BAY-3827 | Kinase | PRKAA1, RPS6KA1 | BAY-974 | No | 01/20 | |
JP3000 | RXRA, RXRB, RXRG | JP3001 | 10/23 | |||
BAY-1797 | Ion channel | P2X4 | BAY-207 | Yes | 11/18 | |
GSK046 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
ABT-724 | GPCR | DRD4 | A-769 | Yes | 05/18 | |
GSM1 | Protease | Gamma secretase complex | GSM-NC | Yes | 05/18 | |
SAFit2 | Isomerase | FKBP5 | ddSAFit2 | Yes | 09/22 | |
BAY-876 | Solute carriers | SLC2A1 | BAY-588 | Yes | 05/18 | |
TP-030-2 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
VZ185 | Bromodomain-containing protein family | BRD7, BRD9 | cisVZ185 | No | 01/24 | |
BAY-293 | Nucleotide exchange factor | SOS1 | BAY-294 | No | 04/19 | |
TP-040 | Hydrolase | OGA | TP-040n | Yes | 09/21 | |
THPP-1 | Phosphodiesterase | PDE10A | THPP-1-NC | Yes | 06/19 | |
JNJ-65355394 | Hydrolase | OGA | JNJ-73924149 | Yes | 11/21 | |
UNC0642 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | Yes | 08/12 | ||
BAY-707 | Hydrolase | NUDT1 | BAY-604 | Yes | 05/18 | |
Skepinone-L | Kinase | MAPK14 | FM-743 | Yes | 01/20 | |
BI-3231 | 17β-hydroxysteroid dehydrogenases | HSD17B13 | BI-0955 | Yes | 09/23 | |
BI 653048 | Nuclear hormone receptor | NR3C1 | BI-3047 | Yes | 11/18 | |
GSK778 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
BAY-7598 | Protease | MMP12 | BAY-694 | Yes | 05/18 | |
MRL-SYKi | Kinase | SYK | MRL-SYKi-NC | Yes | 05/18 | |
JNJ-39758979 | GPCR | HRH4 | JNJ-39668551 | Yes | 09/22 | |
ABT-546 | GPCR | EDNRA | A-545 | Yes | 05/18 | |
(R)-ZINC-3573 | GPCR | MRGPRX2 | (S)-ZINC-3573 | No | 06/20 | |
BAY-6096 | GPCR | ADRA2B | BAY-726 | Yes | 12/23 | |
NI-57 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 12/14 | ||
BI-1230 | Protease | HCV NS3 | BI-1675 | Yes | 03/19 | |
A-446 | Hydrolase | GLS | A-426 | Yes | 07/21 | |
BAY-549 | Kinase | ROCK1, ROCK2 | BAY-4900 | Yes | 06/19 | |
BAY-091 | Kinase | PIP4K2A | BAY-0361 | No | 10/21 | |
GSK343 | Methyltransferase | EZH2 | No | 08/12 | ||
BI-9627 | Solute carriers | SLC9A1 | BI-0054 | Yes | 05/18 | |
BAY-179 | Complex I | BAY-070 | Yes | 01/20 | ||
JNJ-42226314 | Serine hydrolase | MGLL | JNJ-8034 | Yes | 09/23 | |
BI-2545 | Phosphodiesterase | ENPP2 | BI-3017 | Yes | 11/18 | |
BAY-6672 | GPCR | PTGFR | BAY-403 | Yes | 11/20 | |
BAY-474 | Kinase | MET | BAY-827 | Yes | 05/18 | |
A-1211212 | Regulator protein | BCL2 | A-1210227 | Yes | 11/19 | |
BI-2081 | GPCR | FFAR1 | BI-0340 | Yes | 09/22 | |
IOX2 (requires >>> 1 microM for cell assays) |
2OG | PHD2 | No | 02/12 | ||
KISS1-305 | GPCR | KISS1R | KISS1-543 | Yes | 05/18 | |
WM-1119 | Transferase | KAT6A, KAT6B | WM-2474 | Yes | 06/20 | |
BI-8668 | Sodium channels | Epithelial sodium channel (ENaC) | BI-0337 | Yes | 11/23 | |
BI-9564 | Bromodomains | BRD9, BRD7 | Yes | 04/15 | ||
TP-021 | Transcription factor | BCL6 | TP-021n | Yes | 11/18 | |
BI 605906 | Kinase | IKBKB | BI-5026 | Yes | 06/21 | |
CRTH2 antagonist | GPCR | PTGDR2 | CRTH2 negative control | Yes | 05/18 | |
PFI-653 | Hydrolase | VNN1 | PFI-653-N | Yes | 09/21 | |
PFI-1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | No | 11/11 | ||
PF-05105679 | Ion channel | TRPM8 | PF-05257137 | Yes | 05/18 | |
BAY-985 | Kinase | TBK1, IKBKE | BAY-440 | Yes | 01/20 | |
BAY-7081 | Phoshodiesterase | PDE9A | BAY-7424 | Yes | 09/23 | |
BI-4394 | Protease | MMP13 | BI-4395 | Yes | 11/18 | |
BI-2540 | Reverse transcriptase | HIV NNRT | BI-2439 | Yes | 11/20 | |
WEB2086 | GPCR | PTAFR | WEB2387 | Yes | 01/24 | |
MLi-2 | Kinase | LRRK2 | MLi-2-NC | Yes | 05/19 | |
MSD-M1PAM | GPCR | CHRM1 | MSD-M1PAM-NC | Yes | 08/19 | |
TP-050 | Ion channel | GRIN2A | TP-050n | Yes | 09/22 | |
BAZ2-ICR | Bromodomains | BAZ2A, BAZ2B | Yes | 05/14 | ||
ABT-100 | Transferase | FNTB | A-108 | Yes | 05/18 | |
NVS-MALT1 | Protease | MALT1 | NVS-MALT1-C | Yes | 02/20 | |
BI-3802 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
OF-1 | Bromodomains | BRPF1, BRD1, BRPF3 | No | 07/14 | ||
BAY-784 | GPCR | GNRHR | BAY-786 | Yes | 11/18 | |
GSK620 | Bromodomains | BRD2, BRD3, BRD4, BRDT | Yes | 02/21 | ||
BI 665915 | Lipoxygenase | ALOX5AP | BI-0153 | Yes | 05/18 | |
BI-1935 | Hydrolase | EPHX2 | BI-2049 | Yes | 05/18 | |
JNJ-9350 | Oxidase | SMOX | JNJ-4545 | Yes | 09/22 | |
BAY-678 | Protease | ELANE | BAY-677 | Yes | 05/18 | |
BAY-069 | Amino acid transaminase | BCAT1, BCAT2 | BAY-771 | Yes | 09/20 | |
SGK3-PROTAC1 | Kinase | SGK3 | cisSGK3-PROTAC1 | No | 01/24 | |
T3-CLK | Kinase | CLK1, CLK2, CLK3, CLK4 | T3-CLK-N | No | 04/19 | |
JNJ-42396302 | Phosphodiesterase | PDE10A | JNJ-40573663 | Yes | 09/21 | |
MSD-CYP11B2 | Cytochrome P450 | CYP11B2 | MSD-CYP11B2 Negative control | Yes | 06/19 | |
BAY1125976 | Kinase | AKT1/2 | BAY-940 | Yes | 11/21 | |
IOX1 (tool compound) |
2OG | Pan-KDM | No | 01/12 | ||
BAY-386 | GPCR | F2R | BAY-448 | Yes | 05/18 | |
FS-694 | Kinase | MAPK14 | FM-743 | No | 01/20 | |
FHT-2344 | SWI/SNF | SMARCA2, SMARCA4 | FHT-5908 | Yes | 09/23 | |
BI-1950 | Integrin | ITGAL | BI-9446 | Yes | 11/18 | |
GSK789 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK791 | No | 02/21 | |
ERKi | Kinase | MAPK3, MAPK1 | ERKi-NC | Yes | 05/18 | |
MRK-560 | Protease | Gamma secretase complex | GSI-NC | Yes | 05/18 | |
CCT369260 | Transcription factor | BCL6 | CCT393732 | Yes | 09/22 | |
T-26c | Protease | MMP13 | T-26f | Yes | 05/18 | |
TP-030-1 | Kinase | RIPK1 | TP-030n | Yes | 09/20 | |
BAY-277 | Aminopeptidase | METAP2 | BAY-8805 | Yes | 01/24 | |
A-192621 | GPCR | EDNRB | A-1806262 | Yes | 03/19 | |
8RK64 | Regulator protein | UCHL1 | JYQ88 | Yes | 09/21 | |
PPTN | GPCR | P2RY14 | PPTN-NC | Yes | 06/19 | |
Borussertib | Kinase | AKT1, AKT2 | RL2578 | Yes | 10/21 | |
I-CBP112 | Bromodomains | CREBBP, EP300 | No | 03/13 | ||
A-485 | Transferase | EP300, CREBBP | A-486 | Yes | 05/18 | |
SR-318 | Kinase | MAPK14 | SR-321 | No | 01/20 | |
TP-060 | Glucosyltransferase | UGCG | TP-060n | Yes | 09/23 | |
BI 639667 | GPCR | CCR1 | BI-9307 | Yes | 11/18 | |
BAY-3153 | GPCR | CCR1 | BAY-173 | Yes | 02/21 | |
BI 99179 | Synthase | FASN | BI 99990 | No | 05/18 | |
MRL-650 | GPCR | CNR1 | MRL-CB1-NC | Yes | 05/18 | |
JNJ-6204 | Kinase | CSNK1D/CSNK1E | JNJ-0293 | Yes | 09/22 | |
PF-04457845 | Hydrolase | FAAH | PF-04875474 | Yes | 05/18 | |
Ogerin | GPCR | GPR68 | ZINC32547799 | Yes | 06/20 | |
BAY 1753011 | GPCR | AVPR1A, AVPR2 | BAY-2297 | Yes | 12/23 | |
I-BRD9 | Bromodomains | BRD9 | No | 05/15 | ||
TP-024 | GPCR | GPR52 | TP-024n | Yes | 11/18 | |
BI-1942 | Protease | CMA1 | No | 06/21 | ||
MSC-4381 | Monocarboxylate transporter | SLC16A3 | MSC-0516 | Yes | 09/21 | |
Bromosporine (BSP) (tool compound) |
Bromodomains | pan-Bromodomain | No | 01/13 | ||
TP-004 | Protease | METAP2 | TPn-004 | Yes | 05/18 | |
BAY-899 | GPCR | LHCGR | BAY-897 | Yes | 01/20 | |
JNJ-4355 | BCL2 protein family | MCL1 | JNJ-78732576 | Yes | 09/23 | |
BAY-885 | Kinase | MAPK7 | BAY-693 | No | 11/18 | |
BI 207127 | RNA polymerase | HCV NS5B | BI-7656 | Yes | 11/20 | |
BI-5524 | Chymotrypsin | ELANE | BI-5525 | Yes | 01/24 | |
TP-008 | Kinase | ACVR1B, TGFBR1 | Al11 | No | 06/19 | |
IPP/CNRS-A017 | Dehydrogenase | DHODH | IPP/CNRS-A019 | No | 10/19 | |
TP-051 | GPCR | FFAR1 | TP-051n | Yes | 09/22 | |
PFI-4 | Bromodomains | BRPF1 | No | 12/14 | ||
(R)-9s | GPCR | ADRA1D | (S)-9s | Yes | 05/18 | |
SR-302 | Kinase | DDR1, DDR2, MAPK11, MAPK14 | SR-301 | No | 06/20 | |
BI-3812 | Transcription factor | BCL6 | BI-5273 | No | 11/23 | |
TP-020 | Transferase | MGAT2 | TP-020n | Yes | 11/18 | |
GSK973 | Bromodomains | BRD2, BRD3, BRD4, BRDT | GSK943 | Yes | 02/21 | |
BAY-826 | Kinase | TIE1, TEK, DDR1, DDR2 | BAY-309 | Yes | 05/18 | |
JNJ-54119936 | Nuclear hormone receptor | RORC | JNJ-53721590 | Yes | 09/21 | |
GSK-LSD1 | Lysine Demethylase | KDM1A/LSD1 | No | 03/14 | ||
PF-04418948 | GPCR | PTGER2 | PF-04475866 | Yes | 05/18 | |
A-1155463 | Regulator protein | BCL2L1 | A-1107969 | Yes | 11/19 | |
BAY 1816032 | Kinase | BUB1 | BAY-283 | Yes | 10/22 | |
A-079 | Ion channel | TRPA1 | A-226 | Yes | 11/18 | |
BAY-390 | Ion channel | TRPA1 | BAY-9897 | Yes | 09/20 | |
BIBO3304 | GPCR | NPY1R | BIBO3457 | Yes | 01/24 | |
UCSF924 | GPCR | DRD4 | UCSF924NC | Yes | 04/19 | |
JA397 | Kinase | CDK14-18 | JA314 | 07/23 | ||
JQ1 | Bromodomains | BRD2, BRD3, BRD4, BRDT | (-)-JQ1 | Yes | 06/10 | |
PFI-2 | Methyltransferase | SETD7 | (S)-PFI-2 | No | 05/13 | |
LP99 | Bromodomains | BRD9, BRD7 | 2S,3R-enantiomer | No | 12/14 | |
A-196 | Methyltransferase | SUV420H1, SUV420H2 | A-197, SGC2043 | No | 07/15 | |
A-395 | WD40 repeat | EED | A-395N | 07/16 | ||
BAY-299 | Bromodomains | TAF1, BRD1 | BAY-364 | No | 06/16 | |
BAY-598 | Methyltransferase | SMYD2 | BAY-369 | Yes | 04/15 | |
BAY-6035 | Methyltransferase | SMYD3 | BAY-444 | 06/17 | ||
BAY-850 | Bromodomains | ATAD2 | BAY-460 | 01/17 | ||
BAY-805 | USP (ubiquitin specific protease) | USP21 | BAY-728 | No | 10/22 | |
SGC-CBP30 | Bromodomains | CREBBP, EP300 | BDOIA513 | No | 03/13 | |
BI-9321 | Methyl Lysine Binder | NSD3 | BI-9466 | 07/18 | ||
BI01383298 | Solute carriers | SLC13A5 | BI01372674 | 01/18 | ||
CK156 | Kinase | STK17A, DRAK1 | CKJB71 | No | 10/21 | |
CS640 | Kinase | CAMK1 | CS640s | Yes | 01/23 | |
L-Moses | Bromodomains | KAT2A, KAT2B | D-Moses | Yes | 10/17 | |
DDR-TRK-1 | Kinase | DDR, TRK | DDR-TRK-1N | Yes | 08/18 | |
FM-381 | Kinase | JAK3 | FM-479 | 02/17 | ||
GSK-J1 use pro-drug GSK-J4 for cell assays |
Lysine Demethylase | KDM6B/JMJD3, KDM6A/UTX, KDM5B/JARID1B | GSK-J2 (GSK-J5) | No | 07/12 | |
GSK484 | Arginine deiminases | PAD4 | GSK106 | Yes | 03/15 | |
GSK4027 | Bromodomains | KAT2A, KAT2B | GSK4028 | 06/17 | ||
GSK2801 | Bromodomains | BAZ2A, BAZ2B | GSK8573 | Yes | 12/14 | |
GSK8814 | Bromodomains | ATAD2, ATAD2B | GSK8815 | 01/17 | ||
GSK6853 | Bromodomains | BRPF1 | GSK9311 | Yes | 01/17 | |
GSK864 | Dehydrogenase | IDH1 | GSK990 | Yes | 11/15 | |
JA310 | Kinase | MST3, MST4 | JA262 | 11/23 | ||
LLY-283 | Methyltransferase | PRMT5 | LLY-284 | 07/16 | ||
M4K2234 | Kinase | ALK1, ALK2 | M4K2234NC | Yes | 02/22 | |
MRIA9 | Kinase | SIK1, SIK2, SIK3 | MR7 | Yes | 08/21 | |
MRK-740 | Methyltransferase | PRDM9 | MRK-740-NC | 06/18 | ||
MRK-952 | Hydrolase | NUDT5 | MRK-952-NC | No | 10/22 | |
MRK-990 | Methyltransferase | PRMT9, PRMT5 | MRK-990-NC | No | 10/22 | |
MS049 | Methyltransferase | CARM1, PRMT6 | MS049N | No | 06/15 | |
MS023 | Methyltransferase | PRMT1, PRMT3, CARM1, PRMT6, PRMT8 | MS094 | No | 07/15 | |
MSC1186 | Kinase | SRPK | MSC5360 | 01/23 | ||
MU1210 | Kinase | CLK1, CLK2, CLK4, DYRK1A, DYRK1B, DYRK2 | MU140 | No | 05/19 | |
MU1700 | Kinase | ALK1, ALK2 | MU1700NC | Yes | 02/22 | |
MU1742 | Kinase | CK1δ, CK1ε | MU2027 | Yes | 10/22 | |
Homer | WD40 repeat | WDR5 | nc_WDR5 and nc_VHL | No | 07/21 | |
NR162 | Kinase | CASK | NR187 | No | 09/20 | |
NVS-BPTF-1 | Bromodomains | BPTF | NVS-BPTF-C | No | 02/19 | |
NVS-CECR2-1 | Bromodomains | CECR2 | NVS-CECR2-C | No | 06/15 | |
NVS-MLLT-1 | YEATS | MLLT1, MLLT3 | NVS-iMLLT-C | No | 03/20 | |
NVS-PAK1-1 | Kinase | PAK1 | NVS-PAK1-C | No | 06/16 | |
OICR-9429 | WD40 repeat | WDR5 | OICR-0547 | No | 05/14 | |
OICR11029 | Transcription factor | BCL6 | OICR11600 | No | 01/24 | |
PFI-3 | Bromodomains | SMARCA2, PBRM1, SMARCA4 | PFI-3oMet | No | 11/13 | |
PFI-5 | Methyltransferase | SMYD2 | PFI-5N | 07/17 | ||
PFI-6 | YEATS | MLLT1, MLLT3 | PFI-6N | No | 06/20 | |
PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 | |
PFI-8 | YEATS | YEATS | PFI-8N | No | 01/24 | |
SGC-AAK1-1 | Kinase | AAK1, BMP2K, BIKE | SGC-AAK1-1N | 02/18 | ||
SGC-SMARCA-BRDVIII | Bromodomains | PB1(5), SMARCA2/4 | SGC-BRDVIII-NC | 12/20 | ||
SGC-CAF382-1 | Kinase | CDKL5 | SGC-CAF268-1N | 09/23 | ||
SGC-CAMKK2-1 | Kinase | CAMKK1, CAMKK2 | SGC-CAMKK2-1N | No | 01/20 | |
SGC-CDKL5_GSK3 | Kinase | CDKL5, GSK3 | SGC-CDKL5/GSK3-1N | No | 09/23 | |
SGC-GSK3-1 | Kinase | GSK3 | SGC-CDKL5/GSK3-1N | No | 09/23 | |
SGC-CK2-1 | Kinase | CSNK2A1, CSNK2A2 | SGC-CK2-1N | No | 06/20 | |
SGC-CLK-1 | Kinase | CLK1, CLK2, CLK4 | SGC-CLK-1N | No | 02/20 | |
SGC-GAK-1 | Kinase | GAK | SGC-GAK-1N | 02/18 | ||
SGC-PI5P4Kγ/MYLK4-1 | Kinase | PI5P4K gamma, MYLK4 | SGC-PI5P4Kγ/MYLK4-1N | No | 05/23 | |
SGC-PIKFYVE-1 | Kinase | PIKfyve | SGC-PIKFYVE-1N | No | 10/22 | |
SGC-STK17B-1 | Kinase | STK17B, DRAK2 | SGC-STK17B-1N | 02/20 | ||
SGC-UBD1031 | UBD (ubiquitin binding domain) | SGC-UBD1031N | No | 05/24 | ||
SGC-UBD253 | UBD (ubiquitin binding domain) | HDAC6 | SGC-UBD253N | No | 01/22 | |
SGC0946 | Methyltransferase | DOT1L | SGC0649 | No | 08/12 | |
GSK591 | Methyltransferase | PRMT5 | SGC2096 | No | 07/15 | |
SGC3027 | Methyltransferase | PRMT7 | SGC3027N | 03/18 | ||
SGC6870 | Methyltransferase | PRMT6 | SGC6870N | 06/19 | ||
LLY-507 (Multiple Off-target Effects) |
Methyltransferase | SMYD2 | SGC705 | No | 11/13 | |
SGC-CK2-2 | Kinase | CK2/CSNK2 | SGK-CK2-2N | 05/23 | ||
SKI-73 | Methyltransferase | CARM1 | SKI-73N | 07/17 | ||
TH-257 | Kinase | LIMK1, LIMK2 | TH-263 | 07/17 | ||
TH-257 | Kinase | LIMK1, LIMK2 | TH-263 | 07/23 | ||
TP-064 | Methyltransferase | CARM1 | TP-064N | 06/16 | ||
TP-238 | Bromodomains | CECR2, BPTF | TP-422 | 09/18 | ||
TP-472 | Bromodomains | BRD9, BRD7 | TP-472N | Yes | 06/16 | |
UNC0638 | Methyltransferase | EHMT2/G9a, EHMT1/GLP | UNC0737 | No | 06/10 | |
UNC1215 | Methyl Lysine Binder | L3MBTL3 | UNC1079 | No | 08/12 | |
UNC1999 | Methyltransferase | EZH2 | UNC2400 | Yes | 05/13 | |
UNC6934 | Methyl Lysine Binder | NSD2-PWWP1 | UNC7145 | 06/19 | ||
UNC8732 | Methyl Lysine Binder | NSD2 | UNC8884 | No | 01/24 | |
VinSpinIn | Spindlin domains | Spin1 | VinSpinIC | 09/18 | ||
SGC707 | Methyltransferase | PRMT3 | XY1 | No | 06/14 |
Chemical Handles
This versatile modality can be used to develop tools for proximity-inducing chemistry, tracers for target engagement assays, PROTACs, chemical inducers of degradation, and pull-down reagents. Handles bind their target with Kd < 1 micromolar. Their selectivity and cell activity has not been determined.
Chemical Handle | Chemical Probe | Structures | Protein family | Specific Targets | Control | In Vivo Activity* | Added |
---|---|---|---|---|---|---|---|
PFI-E3H1 | PFI-7 | E3 ligase | GID4 | PFI-7N | No | 09/21 |
Please select a protein family