Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and mitosis (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication.

DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. Genome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates.

In cancer cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy.

References:
[1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942.
[2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904.
[3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.
[4] Ghelli Luserna di Rora' A, et al. J Hematol Oncol. 2017 Mar 29;10(1):77.


Anti-infection >
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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
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9-ALPHA-RIBOFURANOSYLADENINE

Alpha-Adenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 5682-25-7
  • MF: C10H13N5O4
  • MW: 267.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 205-207 °C
  • Flash Point: N/A

1,2-Di-O-acetyl-3-deoxy-3-fluoro-5-O-(4-methyl)benzoyl-D-ribofuranose

1,2-Di-O-acetyl-3-deoxy-3-fluoro-5-O-(4-methyl)benzoyl-D-ribofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 1612192-28-5
  • MF: C17H19FO7
  • MW: 354.33
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 440.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.1±23.6 °C

Uridine,2'-chloro-2'-deoxy-5-methyl- (9CI)

2’-Chlorothymidine is a thymidine analogue. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].

  • CAS Number: 54898-34-9
  • MF: C10H13ClN2O5
  • MW: 276.67
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.59g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Divalproex sodium

Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].

  • CAS Number: 76584-70-8
  • MF: C16H31NaO4
  • MW: 310.405
  • Catalog: HIV
  • Density: N/A
  • Boiling Point: 220ºC at 760 mmHg
  • Melting Point: 222ºC
  • Flash Point: 116.6ºC

SMN-C2

SMN-C2 is a close analogs of RG-7916 act as selective RNA-binding ligands that modulate pre-mRNA splicing; directly binds to the AGGAAG motif on exon 7 of the SMN2 pre-mRNA, and promotes a conformational change in two to three unpaired nucleotides at the junction of intron 6 and exon 7 in both in vitro and in-cell models; increases binding of the splicing modulators, far upstream element binding protein 1 (FUBP1) and its homolog, KH-type splicing regulatory protein (KHSRP), to the SMN-C2/C3-SMN2 pre-mRNA complex and enhances SMN2 splicing.

  • CAS Number: 1446311-56-3
  • MF: C24H27N5O2
  • MW: 417.513
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PLK1-IN-4

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma[1].

  • CAS Number: 2622273-55-4
  • MF: C24H25F3N6O4S
  • MW: 550.55
  • Catalog: Polo-like Kinase (PLK)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DMT-2'-O-TBDMS-G(dmf)-CE-phosphoramidite

(2R,3R,4R,5R)-2-((Bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-4-((tert-butyldimethylsilyl)oxy)-5-(2-(((E)-(dimethylamino)methylene)amino)-6-oxo-1,6-dihydro-9H-purin-9-yl)tetrahydrofuran-3-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.

  • CAS Number: 149559-87-5
  • MF: C49H67N8O8PSi
  • MW: 955.16
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BNS-22

BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity[1].

  • CAS Number: 1151668-24-4
  • MF: C24H25NO5
  • MW: 407.459
  • Catalog: Topoisomerase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 622.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 330.4±31.5 °C

Selisistat (EX 527)

Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.

  • CAS Number: 49843-98-3
  • MF: C13H13ClN2O
  • MW: 248.708
  • Catalog: Sirtuin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 531.7±38.0 °C at 760 mmHg
  • Melting Point: 179.0 to 183.0 °C
  • Flash Point: 275.4±26.8 °C

N3-Ethyl pseudouridine

N3-Ethyl pseudouridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2413585-37-0
  • MF: C11H16N2O6
  • MW: 272.25
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FTX-6746

FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models[1].

  • CAS Number: 2829349-96-2
  • MF: C16H7ClF2N2O
  • MW: 316.69
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EMD534085

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.

  • CAS Number: 858668-07-2
  • MF: C25H31F3N4O2
  • MW: 476.534
  • Catalog: Kinesin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 609.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 322.4±31.5 °C

Topoisomerase II inhibitor 8

Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase[1].

  • CAS Number: 2493298-68-1
  • MF: C14H8N4O3S
  • MW: 312.30
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Thiothymidine

2-Thiothymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 28585-51-5
  • MF: C10H14N2O4S
  • MW: 258.29
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.52 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Erythromycin-d3

Erythromycin-d3 is the deuterium labeled Erythromycin[1]. Erythromycin is a macrolide antibiotic produced by actinomycete?Streptomyces erythreus?with a broad spectrum of antimicrobial activity. Erythromycin binds to bacterial 50S ribosomal subunits and inhibits?RNA-dependent protein synthesis?by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid. Erythromycin also exhibits antitumor and neuroprotective effect in different fields of research[2][3][4][5].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-43

Tubulin polymerization-IN-43 (compound 15h) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-43 disrupts cellular microtubule networks by targeting the Colchicine (HY-16569) site, and promots cell cycle arrest of leukemia cells at G2/M phase and cell apoptosis, as well as inhibiting angiogenesis[1].

  • CAS Number: 2773345-90-5
  • MF: C17H13F4N3O
  • MW: 351.30
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amantadine-d6

Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].

  • CAS Number: 1219805-53-4
  • MF: C10H17N
  • MW: 157.29
  • Catalog: Influenza Virus
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2’-Deoxy-N2-cyclopentyl guanosine

2’-Deoxy-N2-cyclopentyl guanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 1353757-90-0
  • MF: C15H21N5O4
  • MW: 335.36
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Deoxy-3’-α-C-methylguanosine

3’-Deoxy-3’-α-C-methylguanosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 444020-69-3
  • MF: C11H15N5O4
  • MW: 281.27
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rencofilstat

Rencofilstat (CRV431) is a non-immunosuppressive analogue of cyclosporine A and pan-cyclophilin inhibitor, potently inhibits cyclophilin isoforms A, B, D, and G with IC50 of 1-7 nM.Rencofilstat (CRV431) is more than 13 times more potent than the parent compound, cyclosporine A (CsA).Rencofilstat (CRV431) inhibits liver HBV DNA and HBsAg, reduces liver HBV DNA levels and moderately decreased serum HBsAg levels in HBV transgenic mouse model.Rencofilstat (CRV431) shows potential as a drug candidate for chronic liver diseases.

  • CAS Number: 1383420-08-3
  • MF: C67H122N12O13
  • MW: 1303.784
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Broxuridine

5-BrdU is a nucleoside analog that competes with thymidine for incorporation into DNA. 5-BrdU is commonly used in the detection of proliferating cells.

  • CAS Number: 59-14-3
  • MF: C9H11BrN2O5
  • MW: 307.098
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 191-194 °C (dec.)(lit.)
  • Flash Point: N/A

Epiblastin A

Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1[1].

  • CAS Number: 16470-02-3
  • MF: C12H10ClN7
  • MW: 287.708
  • Catalog: Casein Kinase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 596.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 314.3±32.9 °C

3’-Deoxy-N6,N6-dimethyladenosine

3’-Deoxy-N6,N6-dimethyladenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 3608-59-1
  • MF: C12H17N5O3
  • MW: 279.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 565.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 295.8±32.9 °C

2’-Deoxy-2’-iodouridine; 2’-Iodo-2’-deoxyuridine

2’-Deoxy-2’-iodouridine; 2’-Iodo-2’-deoxyuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 4753-03-1
  • MF: C9H11IN2O5
  • MW: 354.10
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

n-(9-fluorenylmethoxycarbonyl)-l-leucin&

Fmoc-leucine-15N is a 15N-labeled and 13C-labled EIDD-1931. EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine ence

  • CAS Number: 200937-57-1
  • MF: C21H2315NO4
  • MW: 354.41
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 152-156ºC(lit.)
  • Flash Point: N/A

BAY-0069

BAY-0069 is a potent and selective PPARγ inverse agonist with an IC50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer[1].

  • CAS Number: 420826-65-9
  • MF: C22H16BrN3O4
  • MW: 466.28
  • Catalog: PPAR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3'-Chloro-3'-deoxythymidine

3′-Chloro-3′-deoxythymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 25526-94-7
  • MF: C10H13ClN2O4
  • MW: 260.67
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4’,5’-Didehydro-2’-O-(2-methoxyethyl)uridine

4’,5’-Didehydro-2’-O-(2-methoxyethyl)uridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].

  • CAS Number: 2095417-78-8
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Calcium N5-methyltetrahydrofolate

Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.IC50 value:Target:

  • CAS Number: 26560-38-3
  • MF: C20H23CaN7O6
  • MW: 497.52
  • Catalog: Antifolate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Trimethylapigenin

5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner[1].

  • CAS Number: 5631-70-9
  • MF: C18H16O5
  • MW: 312.31700
  • Catalog: Apoptosis
  • Density: 1.242g/cm3
  • Boiling Point: 506.5ºC at 760mmHg
  • Melting Point: 158-160ºC (dec.)
  • Flash Point: 225.5ºC