|
T18889 |
5-Aminofluorescein
|
5-AF |
Others
|
|
5-Aminofluorescein (5-AF) (5-AF) is a covalently-bound fluorescence marker conjugated with human serum albumin. It exhibits an excitation wavelength of 490 nm and an emission wavelength of 515 nm. |
|
T13858 |
RA190
|
|
Proteasome
|
|
RA190 inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. |
|
T16732 |
Reproxalap
|
NS-2,ADX-102 |
Others
|
|
Reproxalap (NS-2) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal. Reproxalap is a reactive aldehyde species sequestering agent for the treatment of the dry eye. |
|
T7541 |
PTP inhibitor 1
|
PTP Inhibitor II |
Phosphatase
|
|
PTP inhibitor 1 is an inhibitor of cell-permeable protein tyrosine phosphatase (PTP) that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)),with Ki of128 μM. |
|
T13586L |
BPK-29 hydrochloride
|
|
Others
|
|
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein interactions by covalently modifying C274. It impairs the anchorage-independent growth of KEAP1-mutant cancer cel... |
|
T19947 |
EDC hydrochloride
|
EDC-HCl Crosslinker,1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride |
Others
|
|
EDC hydrochloride (EDC-HCl Crosslinker) is a zero-length crosslinker. EDC hydrochloride is ideal for covalently binding proteins or peptides to carboxyl containing beads, resins, or other nanoparticals. |
|
T38960 |
QL-X-138
|
|
Virus Protease
,
MNK
,
BTK
|
|
QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK.The IC 50 s of QL-X-138 against BTK, MNK1 and MNK2 kinases are 9.4 nM, 107.4 nM and 26 nM, respe... |
|
T10460 |
Batabulin
|
T138067 |
Apoptosis
,
Microtubule Associated
|
|
Batabulin (T138067) is an antitumor compound, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to ce... |
|
T77762 |
ROS-generating agent 1
|
|
Apoptosis
,
Ferroptosis
,
ROS Kinase
|
|
Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and... |
|
T5674 |
H-151
|
|
STING
|
|
H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammator... |
|
T21320 |
Methoxyamine HCl
|
TRC102,TRC 102,Methoxyamine,TRC-102 |
Others
|
|
Methoxyamine HCl (Methoxyamine) covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. Methoxyamine is... |
|
T3215 |
JNJ-42165279
|
JNJ42165279 |
FAAH
,
Autophagy
|
|
JNJ-42165279 covalently inactivates the FAAH enzyme but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 (10 μM) exhibits high selectivity against a panel of 50 re... |
|
TQ0236 |
Tirabrutinib
|
ONO-4059,GS-4059,Velexbru |
BTK
|
|
Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and ... |
|
T7084 |
2-Bromo-4'-hydroxyacetophenone
|
SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide |
Phosphatase
|
|
2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SH... |
|
T0668 |
1-Aminohydantoin hydrochloride
|
|
Others
|
|
1-Aminohydantoin hydrochloride is a major metabolite of furantoin in animal tissues. It is covalently bound to tissue proteins, released from tissues under slightly acidic conditions, and can be detected by derivatizatio... |
|
T6446 |
Clevudine
|
L-FMAU,Levovir |
HBV
,
DNA/RNA Synthesis
|
|
Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The ... |
|
T36256 |
LC-2
|
LC 2,PROTAC KRASG12C Degrader-LC-2,LC2 |
PROTACs
|
|
LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a PROTAC that covalently binds KRAS G12C with MRTX849 and recru... |
|
T21687 |
Conoidin A
|
|
Parasite
|
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. It covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation ... |
|
T11191 |
EN6
|
|
Proton pump
,
Autophagy
|
|
EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative ... |
|
T38960L |
QL-X-138 HCl
|
QL-X-138 HCl（1469988-63-3 Free base） |
MNK
,
BTK
|
|
QL-X-138 HCl is a novel selective and highly potent BTK/MNK dual-kinase inhibitor with anticancer activity that binds covalently to BTK and noncovalently to MNK. QL-X-138 HCl inhibited BTK, MNK1, and MNK2 kinases. QL-X-1... |
|
T3024 |
Avitinib
|
AC0010 |
EGFR
,
JAK
,
BTK
|
|
Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administrat... |
|
T27391 |
FSBA
|
|
|
|
FSBA inhibits covalently anthrax edema factor. |
|
T35061 |
Vinthionine
|
L-Vinthionine,S-Ethenyl-L-homocysteine |
|
|
Vinthionine binds covalently to rat liver DNA, RNA, and protein in vivo, but not in vitro. |
|
T28389 |
PF-6422899
|
PF6422899,PF 6422899 |
|
|
PF-6422899 irreversibly inhibits EGFR kinase activity by binding covalently to active-site cysteine residues in the ATP binding pocket of EGFR. |
|
T29596 |
Acetylaminofluorene-dG
|
dG-8-AAF,8-AAF dG,8 AAF-dG,8-AAF-dG |
|
|
Acetylaminofluorene-dG is a carcinogenic adduct which covalently binds DNA bases and promotes mutagenesis near the adduct site. |
|
T15626 |
JPM-OEt
|
|
Others
|
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor with antitumor activity. JPM-OEt binds covalently in the active site and irreversibly inhibits the cysteine cathepsin family. |
|
TP2303 |
ZIP, Biotinylated
|
|
Others
|
|
ZIP with a biotin moiety covalently attached |
|
T30461 |
BI-RJ 70
|
BI RJ 70,BIRJ70,BI-RJ-70 |
|
|
BI-RJ 70 is a tritiated photoaffinity azide analog of nevirapine, which can be used to study the binding of nevirapine to HIV-1 transcriptase through covalently labeled enzymes and amino acid residues. |
|
T11956L |
MBC-11
|
|
Others
|
|
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). It also has the potential to treat tumor-induced bone disease (TIBD). |
|
T27200 |
DOX−NOP1 HCl
|
doxorubicin-NOP1 conjugate,doxorubicin-NOP1 HCl,DOX−NOP1 Hydrochloride |
|
|
DOX−NOP1 is a molecular hybrid covalently joining doxorubicin (DOX) and NOP1. DOX−NOP1 showed similar increased toxicity toward resistant cancer cells and, in addition, lower cardiotoxicity than DOX. |
|
T27766 |
Hymeglusin
|
L659,699,L 659,699,L-659,699 |
|
|
L-659,699, also known as hymeglusin, is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme. |
|
T33957 |
PF-Alkyne
|
PF Alkyne |
|
|
PF-Alkyne is a fluorophosphonate-based probe which specifically and covalently reacts with the tyrosine-111 residue of the Schistosoma japonicum GST (sjGST) tag. PF-Alkyne rapidly and site-selectively immobilizes sjGST f... |
|
T17060 |
Tetramethylrhodamine-5-iodoacetamide
|
5-TMRIA |
Others
|
|
Tetramethylrhodamine-5-iodoacetamide (5-TMRIA) is a thiol-selective reactive dye that is used to non-specifically label proteins via the cysteine residues and covalently label DNA fragments[1]. |
|
T21318 |
Efaproxiral
|
RSR13,Efaproxyn,RSR 13,RSR-13 |
|
|
Efaproxiral is a synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen... |
|
T73006 |
Cis-ccc_R08
|
|
|
|
cis-ccc_R08 infection . cis-ccc_R08 is a cccDNA (covalently closed circular DNA) inhibitor . |
|
T13586 |
BPK-29
|
|
Others
|
|
|
|
T16327 |
Nitracrine
|
|
Others
|
|
Nitracrine is a 1-nitroacridine derivative and is an effective hypoxia-selective agent in vitro and antitumor drugs. Nitracrine suppresses RNA synthesis and covalently, reversibly binds to DNA but also forms covalent add... |
|
T41056 |
Phalloidin-TRITC
|
|
|
|
Phalloidin-TRITC is a TRITC labeled, red fluorescence probe for F-actin . Phalloidin, bound to actin filaments, reacts covalently with amino acids Glu-llT, Met-ll9, and Met355, which are very close to the nucleotide bind... |
|
T11956 |
MBC-11 triethylamine
|
|
Others
|
|
MBC-11 triethylamine has potential to treat tumor-induced bone disease (TIBD), is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). |
|
T16568 |
PR-924
|
|
Proteasome
|
|
PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-92... |
|
T75139 |
TMX1
|
|
|
|
TMX1 is a molecular glue degrader that covalently targets BRD4. It selectively recruits DCAF16 to the BRD4 BD2 domain, leading to the degradation of BRD4 [1]. |
|
T11957 |
MBC-11 trisodium
|
|
Others
|
|
MBC-11 trisodium has potential to treat tumor-induced bone disease (TIBD).It is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. |
|
T62534 |
POP-IN-2
|
|
|
|
POP-IN-2 (Compound 7k) is a potent, covalently bound inhibitor of prolyl oligopeptidase (POP) (Ki: 6 nM).POP-IN-2 can be used in neurodegenerative disease and cancer research. |
|
TP1837 |
Acyl Carrier Protein (ACP) (65-74)
|
Acyl Carrier Protein (ACP) 65-74 |
|
|
Acyl Carrier Protein (ACP) (65-74) is an active acyl carrier protein (ACP) fragment.Acyl Carrier Protein (ACP) is a component of plastid-located plant fatty acid synthetase. It binds acyl groups covalently via the prosth... |
|
T72328 |
Cyclopropenone probe 1
|
|
|
|
Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1) , by covalently binding at the catalytic active site. |
|
T74026 |
AUTAC2
|
|
|
|
AUTAC2, an autophagy-mediated degrader (AUTAC) targeting FKBP12, comprises an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. The SLF component binds non-covalently to FKBP12 [1]. |
|
T70403 |
VUF14480
|
|
|
|
VUF14480 is a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. VUF14480 was shown to be a partial agonist of hH4 receptor-mediated G protein signalling and β-arrestin2 re... |
|
T63704 |
FGFR4-IN-11
|
|
|
|
FGFR4-IN-11 is a selective, potent, covalently bound FGFR4 inhibitor (IC50: 2.1 nM). FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and exhibits anticancer effects. |
|
T73282 |
HBV-IN-31
|
|
|
|
HBV-IN-31, a potent inhibitor of covalently closed circular DNA (cccDNA), demonstrates significant anti-HBV activity by inhibiting cell growth and exhibiting an IC50 value of 0.13 µM for HBsAg. |
|
T73283 |
HBV-IN-32
|
|
|
|
HBV-IN-32, a potent inhibitor of covalently closed circular DNA (cccDNA), exhibits significant anti-Hepatitis B Virus (HBV) activity by achieving an IC50 of 0.14 µM against HBsAg. Additionally, it impedes cell growth. |
