| DC45827 |
BTO-1 |
BTO-1 is a Polo-like kinase (Plk) inhibitor. BTO-1 is primarily used for phosphorylation and dephosphorylation applications. |
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| DC45861 |
CDK12-IN-2
Featured
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CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12. |
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| DC45897 |
Volasertib trihydrochloride |
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models. |
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| DC45918 |
LY243246 |
LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis. |
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| DC45986 |
Hippeastrine |
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities. |
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| DC46049 |
Ribociclib D6 hydrochloride |
Ribociclib D6 (LEE011 D6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex. |
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| DC46050 |
Lurbinectedin D3 |
Lurbinectedin D3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively. |
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| DC46167 |
Sovesudil |
Sovesudil, formally known as PHP-201, is a well-tolerated and low toxicity Rho-associated protein kinase (ROCK) inhibitor. Sovesudil can be used for the research of normal-tension glaucoma (NTG). |
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| DC46261 |
CDK7-IN-2 hydrochloride hydrate |
CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity. |
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| DC46282 |
CDK4/6-IN-5 |
CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. (from patent WO2019207463A1 example A93). |
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| DC46283 |
Sibiromycin
Featured
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Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine. |
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| DC46338 |
CD532 hydrochloride |
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
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| DC46359 |
PF-07104091 hydrate |
PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2). |
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| DC46399 |
ZN-c3
Featured
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ZN-c3 is an orally active, highly potent and selective Wee1 inhibitor (IC50=3.9 nM). ZN-c3 can be used for the research of cancer. |
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| DC46428 |
PARP1-IN-5 dihydrochloride |
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer. |
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| DC46429 |
PARP1-IN-5 |
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer. |
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| DC46430 |
PF-3758309 dihydrochloride |
PF-3758309 dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation. |
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| DC46439 |
CDK12-IN-4 |
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1). |
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| DC46440 |
CDK12-IN-5 |
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1). |
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| DC46441 |
CDK12-IN-6 |
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1). |
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| DC46459 |
3-Methylthienyl-carbonyl-JNJ-7706621 |
3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer. |
|
| DC46470 |
CPS2 |
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia. |
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| DC46480 |
RKI-1447 dihydrochloride |
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis. |
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| DC46491 |
BAY-8400
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BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 81 nM. BAY-8400 shows synergistic activity of DNA-PK inhibition when combined with DNA damage inducing cancer therapy, like targeted alpha radiation. |
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| DC46497 |
CDK8-IN-1 |
CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM. |
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| DC46526 |
5-Iminodaunorubicin |
5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells. |
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| DC46538 |
2-Amino-2'-deoxyadenosine |
2-Amino-2'-deoxyadenosine is a deoxyribonucleoside used for the oligonucleotide synthesis. |
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| DC46539 |
5'-O-DMT-2'-O-TBDMS-Bz-rC |
5'-O-DMT-2'-O-TBDMS-Bz-rC is a modified nucleoside and can be used to synthesize DNA or RNA. |
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| DC46540 |
5'-O-DMT-2'-O-TBDMS-rI |
5'-O-DMT-2'-O-TBDMS-rI is a modified nucleoside. 5'-O-DMT-2'-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid. |
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| DC46541 |
5'-O-DMT-N2-DMF-dG |
5'-O-DMT-2'-O-TBDMS-rI is a modified nucleoside. 5'-O-DMT-2'-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid. |
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