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Results for "

Selective CDK inhibitors

" in MedChemExpress (MCE) Product Catalog:

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研究分野別:	Cancer (292) Cardiovascular Disease (3) Infection (12) Inflammation/Immunology (23) Metabolic Disease (7) Neurological Disease (20)
クリックケミストリー:	Alkynes (2)

323

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Targets Recommended: CDK Serpin

製品番号	製品名	Target	研究分野	構造式

HY-16297A

Abemaciclib 115+ Cited Publications LY2835219	CDK	Neurological Disease Cancer
Abemaciclib (LY2835219) is a selective and BBB-permeable *CDK4/6* inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-12529

Ro-3306 65+ Cited Publications	CDK Apoptosis	Cancer
Ro-3306 is a potent and selective inhibitor of *CDK1, with K_is of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK*2/cyclin E, respectively.

HY-16297

Abemaciclib methanesulfonate 115+ Cited Publications LY2835219 methanesulfonate	CDK	Cancer
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective and BBB-permeable *CDK4/6* inhibitor with IC₅₀s of 2 nM and 10 nM for CDK4 and CDK6, respectively .

HY-103712A

Samuraciclib hydrochloride 10+ Cited Publications CT7001 hydrochloride; ICEC0942 hydrochloride	CDK Apoptosis	Cancer
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .

HY-158106

AZD8421 1 Publications Verification	CDK	Cancer
AZD8421 is a selective *CDK2* inhibitor (IC₅₀ = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer .

HY-80013

THZ1 90+ Cited Publications	CDK	Cancer
THZ1 is a selective and potent covalent *CDK7* inhibitor with an IC₅₀ of 3.2 nM. THZ1 also inhibits the closely related kinases *CDK12* and *CDK13* and downregulates MYC expression .

HY-101257

YKL-5-124 15+ Cited Publications	CDK	Cancer
YKL-5-124 is a potent, selective, irreversible and covalent *CDK7* inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for *CDK7* and *CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective* for *CDK7* than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

HY-103618

THZ531 35+ Cited Publications	CDK	Cancer
THZ531 is a selective and covalent inhibitor of both *CDK12* and *CDK13* with IC₅₀s of 158 nM and 69 nM, respectively .

HY-112272

Lerociclib 2 Publications Verification G1T38	CDK	Cancer
Lerociclib (G1T38) is a potent and selective inhibitor of *CDK4/6, with IC₅₀s* of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

HY-103712

Samuraciclib 10+ Cited Publications CT7001; ICEC0942	CDK Apoptosis	Cancer
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .

HY-137478

KB-0742 3 Publications Verification	CDK	Cancer
KB-0742 is a potent, selective and orally active *CDK9* inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .

HY-101611

MSC2530818 3 Publications Verification	CDK	Cancer
MSC2530818 is a potent, selective and orally available *CDK8* inhibitor with an IC₅₀ of 2.6 nM for CDK8.

HY-10014

R547 2 Publications Verification	CDK GSK-3 Apoptosis	Cancer
R547 is a potent, selective and orally active ATP-competitive *CDK* inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .

HY-117535

CDK2-IN-4 3 Publications Verification	CDK	Cancer
CDK2-IN-4 (compound 73) is a potent and selective *CDK2* inhibitor with an IC₅₀ of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC₅₀=86 uM) .

HY-11009

CGP60474 5+ Cited Publications	CDK PKC	Cancer
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC₅₀ values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .

HY-111388B

Romaciclib hydrochloride 5+ Cited Publications SEL120-34A hydrochloride	CDK	Cancer
SEL120-34A hydrochloride is a potent, selective, orally available, ATP-competitive *CDK8* inhibitor, with IC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

HY-122586

BRD6989 2 Publications Verification	CDK Interleukin Related	Inflammation/Immunology
BRD6989, an analog of the natural product cortistatin A (dCA), inhibits *CDK8* and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC₅₀ of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes .

HY-16297AR

Abemaciclib (Standard) LY2835219 (Standard)	Reference Standards CDK	Cancer
Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective and BBB-permeable *CDK4/6* inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-168162

ZLC491	PROTACs CDK	Cancer
ZLC491 is an orally active PROTAC degrader that selectively targets *CDK12/CDK13* and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of *CDK12* and *CDK13. ZLC491 inhibits* the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer .

HY-112626

CDK12-IN-2 1 Publications Verification	CDK	Cancer
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 .

HY-13266A

BS-181 hydrochloride 5+ Cited Publications	CDK	Cancer
BS-181 hydrochloride is a highly selective *CDK7* inhibitor with IC₅₀ of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

HY-137478A

KB-0742 dihydrochloride 3 Publications Verification	CDK	Cancer
KB-0742 dihydrochloride is a potent, selective and orally active *CDK9* inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity .

HY-16297AS

Abemaciclib-d8 LY2835219-d₈	CDK	Cancer
Abemaciclib-d₈ is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-18299

Purvalanol B 2 Publications Verification NG 95	CDK Parasite	Infection Cancer
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor *CDK, with IC₅₀s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity* for CDK over a range of other protein kinases (IC₅₀>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .

HY-80013A

THZ1 Hydrochloride 90+ Cited Publications	CDK	Cancer
THZ1 Hydrochloride is a selective and potent covalent *CDK7* inhibitor with an IC₅₀ of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases *CDK12* and *CDK13* and downregulates MYC expression .

HY-148214

CDK2/4/6-IN-2	CDK	Cancer
CDK2/4/6-IN-2 is a selective *CDK2/4/6* inhibitor with IC₅₀ values <1 μM. CDK2/4/6-IN-2 inhibits cells proliferation and phosphorylation of retinoblastoma protein at Ser807/811 in breast cancer cells. CDK2/4/6-IN-2 can be used for the research of cancer, such as breast cancer .

HY-12871B

Atuveciclib 5+ Cited Publications BAY-1143572	CDK	Cancer
Atuveciclib (BAY-1143572) is a potent and highly selective, oral *PTEFb/CDK9* inhibitor. Atuveciclib (BAY-1143572) inhibits *CDK9/CycT1* with an IC₅₀ of 13 nM .

HY-111388

SEL120-34A 5+ Cited Publications	CDK	Cancer
SEL120-34A is a potent, selective, orally available, ATP-competitive *CDK8* inhibitor, with IC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

HY-124639

CDK9 inhibitor HH1	CDK	Cancer
CDK9 inhibitor HH1 is a potent and selectively *CDK9* inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer .

HY-112261

CDK12-IN-3 1 Publications Verification	CDK	Cancer
CDK12-IN-3 is a potent and selective *CDK12* inhibitor with an IC₅₀ of 491 nM in enzymatic assay.

HY-112460

CDK2-IN-3	CDK	Cancer
CDK2-IN-3 (compound 3) is a potent and selective *CDK2* inhibitor with an IC₅₀ of 60 nM .

HY-111427

CDK8/19-IN-1	CDK	Cancer
CDK8/19-IN-1 is a potent, selective and oral bioavailable *CDK8/19* dual inhibitor, with IC₅₀s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

HY-13231

CDK9-IN-1 1 Publications Verification	CDK HIV	Infection
CDK9-IN-1 is a novel, selective *CDK9* inhibitor for the treatment of HIV infection, with an IC₅₀ of 39 nM for CDK9/CycT1, extracted from reference, compound 87.

HY-117203A

CDK12-IN-E9 1 Publications Verification	CDK	Cancer
CDK12-IN-E9 is a potent and selective covalent *CDK12* inhibitor and a non-covalent *CDK9* inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC₅₀> 1 μM .

HY-145072

BSJ-01-175	CDK	Cancer
BSJ-01-175 is a potent and selective *CDK12/13* covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .

HY-103492

CDK8-IN-1	CDK	Cancer
CDK8-IN-1 is a potent and selective *CDK8* inhibitor with an IC₅₀ of 3 nM.

HY-102039

CDK9-IN-8	CDK	Cancer
CDK9-IN-8 is a highly effective and selective *CDK9* inhibitor with an IC₅₀ of 12 nM.

HY-46568

CDK7/12-IN-1	CDK	Cancer
CDK7/12-IN-1 is a selective *CDK7/12* inhibitor with IC₅₀s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth .

HY-151463

CDK8-IN-11	Wnt CDK β-catenin	Cancer
CDK8-IN-11 is a potent and selective *CDK8* inhibitor with an IC₅₀ value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer .

HY-139980

CDK9-IN-13	CDK	Cancer
CDK9-IN-13 (compound 38) is potent and selective *CDK9* inhibitor, with an IC₅₀ of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents .

HY-112462

Cdk1/2 Inhibitor III	CDK	Cancer
Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC₅₀s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC₅₀ of 32 nM), GSK-3β (IC₅₀ of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC₅₀s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively .

HY-112272A

Lerociclib dihydrochloride 2 Publications Verification G1T38 dihydrochloride	CDK	Cancer
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of *CDK4/CDK6*, with IC₅₀s of 1 nM and 2 nM for *CDK4/CyclinD1* and *CDK6/CyclinD3*, respectively.

HY-162255

CDK2-IN-23	CDK	Cancer
CDK2-IN-23 (Compound 17) is a kinase selective and highly potent *CDK2* inhibitor (IC₅₀ = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .

HY-103712C

Samuraciclib hydrochloride hydrate 10+ Cited Publications CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate	CDK Apoptosis	Cancer
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .

HY-103712B

Samuraciclib hydrochloride dihydrate 10+ Cited Publications CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate	CDK Apoptosis	Cancer
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .

HY-155218

TMX-2172	PROTACs CDK	Cancer
TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual *CDK2* and *CDK5* degrader with IC₅₀ values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .

HY-101257B

YKL-5-124 TFA 15+ Cited Publications	CDK	Cancer
YKL-5-124 TFA is a potent, selective, irreversible and covalent *CDK7* inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for *CDK7* and *CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective* for *CDK7* than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

HY-145693

CDK5-IN-2	CDK	Others
CDK5-IN-2 (compound 15) is a highly selective *CDK5* inhibitor with IC₅₀s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively .

HY-147600

CDK7-IN-15	CDK	Cancer
CDK7-IN-15 (Compound 8) is a selective *CDK7* inhibitor with an IC₅₀ greater than 10 nM and less than or equal to 100 nM. CDK7-IN-15 is applicable to the research of cancers associated with transcriptional dysregulation .

HY-114903

(E/Z)-BIO-acetoxime GSK-3 Inhibitor X	GSK-3 CDK	Neurological Disease Metabolic Disease Cancer
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC₅₀ of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over *CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC₅₀*=2.4, 4.3, 63 μM) .

製品番号	製品名	構造式

HY-16297AS

Abemaciclib-d8
Abemaciclib-d₈ is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-50767S

Palbociclib-d8
Palbociclib-d₈ is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

HY-129336S

Abemaciclib metabolite M20-d8
Abemaciclib metabolite M20-d₈ is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor .

HY-151580S

CDK2-IN-14-d3
CDK2-IN-14-d₃ is a potent and selective CDK2 inhibitor. CDK2-IN-14-d₃ can be used in research of cancer .

HY-W654305

Palbociclib-d4

Palbociclib-d₄ is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .

HY-176174S

CDK2-IN-46
CDK2-IN-46 (compound 5g) is a selective *CDK2* inhibitor with an IC₅₀ of 0.3 nM. CDK2-IN-46 has a selectivity of >200-fold for CDK1, CDK7, CDK9, CDK4, and CDK6. CDK2-IN-46 shows improves rat and cyno pharmacokinetic profiles .

HY-50767S1

Palbociclib-d4 hydrochloride
Palbociclib-d₄ (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC₅₀s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .

製品番号	製品名		Classification

HY-116423

JH295		Alkynes
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-116423A

JH295 hydrate		Alkynes
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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