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 >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
Cell Cycle/DNA Damage >
Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
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ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
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
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

Tubulin polymerization-IN-26

Tubulin polymerization-IN-26 (compound 12h) can inhibit the polymerization of microtubulin by binding to the colchicine binding site of microtubulin with an IC50 value of 4.64 μM. Tubulin polymerization-IN-26 can induce apoptosis and inhibit cell metastasis or migration, and can be used as a potential compound for lung cancer research[1].

  • CAS Number: 2490291-68-2
  • MF: C25H23N3O2
  • MW: 397.47
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Amino-3’-deoxy-5-methyl uridine

3’-Amino-3’-deoxy-5-methyl uridine, Anticancer antiviral agent 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: 108630-07-5
  • MF: C10H15N3O5
  • MW: 257.24
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-Azido-3’-deoxyuridine

3’-Azido-3’-deoxyuridine 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: 70580-88-0
  • MF: C9H11N5O5
  • MW: 269.21
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SIRT5 inhibitor

SIRT5 inhibitor is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.

  • CAS Number: 2166487-21-2
  • MF: C31H39FN6O6S2
  • MW: 674.81
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5'-O-TBDMS-dA

5'-O-TBDMS-dA is a modified nucleoside and can be used to synthesize DNA or RNA.

  • CAS Number: 51549-30-5
  • MF: C16H27N5O3Si
  • MW: 365.50300
  • Catalog: DNA/RNA Synthesis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cdc7-IN-14

Cdc7-IN-14 (compound 82) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-14 has the potential for the research of cancer[1].

  • CAS Number: 2764866-21-7
  • MF: C18H20N4O2S
  • MW: 356.44
  • Catalog: CDK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CKI-7 HCl

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].

  • CAS Number: 1177141-67-1
  • MF: C11H14Cl3N3O2S
  • MW: 358.67200
  • Catalog: Casein Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Edatrexate

Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck[1][2].

  • CAS Number: 80576-83-6
  • MF: C22H25N7O5
  • MW: 467.47800
  • Catalog: Antifolate
  • Density: 1.441 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Amino-6-bromo-5-cyano-1-(beta-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine

4-Amino-6-bromo-5-cyano-1-(beta-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine is a pyrimidine nucleoside analog. Pyrimidine nucleoside analogs have a wide range of biochemical and anticancer activities. These include DNA synthesis inhibition, RNA synthesis inhibition, antiviral effects, and immunomodulatory effects[1].

  • CAS Number: 1203470-58-9
  • MF: C12H12BrN5O4
  • MW: 370.16
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Iminodaunorubicin

5-Iminodaunorubicin hydrochloride is a quinone-modified anthracycline that retains antitumor activity[1]. 5-Iminodaunorubicin hydrochloride produces protein-concealed DNA strand breaks in cancer cells[2].

  • CAS Number: 67324-99-6
  • MF: C27H31ClN2O9
  • MW: 562.99600
  • Catalog: DNA/RNA Synthesis
  • Density: 1.51g/cm3
  • Boiling Point: 864.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 476.9ºC

(1S)-1,4-Anhydro-1-C-(2,4-difluoro-5-methylphenyl)-D-ribitol

(1S)-1,4-Anhydro-1-C-(2,4-difluoro-5-methylphenyl)-D-ribitol 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: 875302-27-5
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rho Kinase Inhibitor III,Rockout

3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC50 of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay[1].

  • CAS Number: 7272-84-6
  • MF: C13H10N2
  • MW: 194.23200
  • Catalog: ROCK
  • Density: 1.211g/cm3
  • Boiling Point: 406.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 185.2ºC

Thiarabine

Thiarabine (OSI-7836) shows potent anti-tumor activity and inhibition of DNA synthesis.

  • CAS Number: 26599-17-7
  • MF: C9H13N3O4S
  • MW: 259.282
  • Catalog: DNA/RNA Synthesis
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 535.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 277.4±32.9 °C

3’-Deoxy-3’,5-difluorocytidine

3’-Deoxy-3’,5-difluorocytidine 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: 661470-65-1
  • MF:
  • MW:
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-O-MOE-N6-Bz-rA

N6-Benzoyl-2'-O-(2-methoxyethyl)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: 333335-93-6
  • MF: C20H23N5O6
  • MW: 429.43
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ATRA-biotin

ATRA-biotin (Biotin-ATRA-conjugate) is a biotin-conjugated ATRA. ATRA-biotin can be used to track ATRA in cells or a given tissue[1].

  • CAS Number: 2226143-93-5
  • MF: C36H55N3O4S
  • MW: 625.90
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3’-β-C-Ethynyladenosine

3’-β-C-Ethynyladenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].

  • CAS Number: 180300-54-3
  • MF: C12H13N5O4
  • MW: 291.26
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amsacrine

Amsacrine is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

  • CAS Number: 51264-14-3
  • MF: C21H19N3O3S
  • MW: 393.459
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 563.0±60.0 °C at 760 mmHg
  • Melting Point: 230-240ºC
  • Flash Point: 294.3±32.9 °C

Levofloxacin hydrochloride

Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research[1][2][3][4].

  • CAS Number: 177325-13-2
  • MF: C18H21ClFN3O4
  • MW: 397.828
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: 571.5ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 299.4ºC

1,4-Anhydro-2,3-O-isopropylidene-5-O-t-butyldiphenylsilyl-4-thio-D-ribitol

1,4-Anhydro-2,3-O-isopropylidene-5-O-t-butyldiphenylsilyl-4-thio-D-ribitol 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: 1320269-77-9
  • MF: C24H32O3SSi
  • MW: 428.66
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PBK-IN-9

PBK-IN-9 (compound 1160) is a potent PDZ binding kinase (PBK) inhibitor[1].

  • CAS Number: 1338540-55-8
  • MF: C20H18N2O2S
  • MW: 350.434
  • Catalog: TOPK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 498.7±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 255.4±28.7 °C

AR-13503

AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1][2].

  • CAS Number: 1254032-16-0
  • MF: C19H19N3O2
  • MW: 321.37
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chktide

Chktide is a substrate for CHK1 and CHK2. Chktide can be used in kinase assays[1][2].

  • CAS Number: 289652-77-3
  • MF: C115H198N40O33S
  • MW: 2701.12
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW843682X

GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ∼30 other kinases.

  • CAS Number: 660868-91-7
  • MF: C22H18F3N3O4S
  • MW: 477.46
  • Catalog: Polo-like Kinase (PLK)
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 629.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 334.6±34.3 °C

CX-4945 (sodium salt)

CX-4945 sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

  • CAS Number: 1309357-15-0
  • MF: C19H11ClN3NaO2
  • MW: 371.75200
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N6-Phenoxyacetyladenosine

N-(2-Phenoxyacetyl)adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].

  • CAS Number: 119824-65-6
  • MF: C18H19N5O6
  • MW: 401.37
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-[3-[(Trifluoroacetyl)amino]propyl]uridine

5-[3-[(Trifluoroacetyl)amino]propyl]uridine 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: 327623-80-3
  • MF: C14H18F3N3O7
  • MW: 397.30
  • Catalog: Nucleoside Antimetabolite/Analog
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Folic Acid

Folic acid(Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.

  • CAS Number: 59-30-3
  • MF: C19H19N7O6
  • MW: 441.397
  • Catalog: DNA/RNA Synthesis
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 250 °C
  • Flash Point: N/A

Benzoic acid,2-[[[(4S)-4-carboxy-4-[[4-[[(2,4-diamino-6-pteridinyl)methyl]amino]benzoyl]amino]butyl]amino]carbonyl]-

Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth[1][2].

  • CAS Number: 113857-87-7
  • MF: C27H27N9O6
  • MW: 573.56000
  • Catalog: Antifolate
  • Density: 1.51g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMVC2

BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer[1].

  • CAS Number: 850559-51-2
  • MF: C28H25I2N3
  • MW: 657.33
  • Catalog: G-quadruplex
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A