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Isoforms Recommended:	CDK12

Results for "

CDK12

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) CDK (50) DNA/RNA Synthesis (2) GSK-3 (1) HDAC (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (7) PARP (2) PROTACs (10) Raf (1) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (50) Metabolic Disease (1)
Oligonucleotides:	Rat Pre-designed siRNA Sets (1) Mouse Pre-designed siRNA Sets (1) Human Pre-designed siRNA Sets (1) siRNAs (3)

Inhibitors & Agonists

Recombinant Proteins

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-112626

CDK12-IN-2	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-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-RS02356

CDK12 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA) CDK	Others
CDK12 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK12 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK12 Human Pre-designed siRNA Set A CDK12 Human Pre-designed siRNA Set A

HY-RS02358

Cdk12 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA) CDK	Others
Cdk12 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdk12 Rat Pre-designed siRNA Set A Cdk12 Rat Pre-designed siRNA Set A

HY-RS02357

Cdk12 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA) CDK	Others
Cdk12 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdk12 Mouse Pre-designed siRNA Set A Cdk12 Mouse Pre-designed siRNA Set A

HY-162528

CDK12-IN-7	CDK	Cancer
CDK12-IN-7 (Compound 2) is a *CDK12* and *CDK2* inhibitor with IC₅₀ values of 42 and 196 nM, respectively. CDK12-IN-7 has anti-cell proliferation activity and can be used in cancer research .

HY-160284

CDK12/13-IN-1	CDK	Cancer
CDK12/13-IN-1 (Compound 4) is a *CDK12/13* inhibitor. CDK12/13-IN-1 has antitumor activity .

HY-173042

CDK12/13-IN-2	CDK	Cancer
CDK12/13-IN-2 (Compound 24) is a covalent inhibitor of *CDK12/13, with IC₅₀* values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. CDK12/13-IN-2 can inhibit the proliferation of breast cancer cells and can be used in the research of triple-negative breast cancer .

HY-168658

CDK12/13 ligand 2	Ligands for Target Protein for PROTAC	Cancer
CDK12/13 ligand 2 is a potent *CDK12* and *CDK13* ligand. CDK12/13 ligand 2 can be used to synthesize YJ1206 (HY-168555) .

HY-139328

CDK12-IN-5	CDK	Cancer
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) .

HY-139329

CDK12-IN-6	CDK	Cancer
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) .

HY-139327

CDK12-IN-4	CDK	Cancer
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) .

HY-173059

CDK12/13-IN-3	CDK	Cancer
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for *CDK* that inhibits *CDK12* and *CDK13* with IC₅₀ of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC₅₀ of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .

HY-168163

CDK12/13 ligand 1	CDK	Cancer
ALK-IN-29 (compound 4c) has a certain inhibitory effect on tyrosine protein kinases ALK, *CDK2/CyclinE1* and FAK, among which the strongest inhibitory effect on ALK kinase is 40.63% at a concentration of 10 μM. ALK-IN-29 can be used for anti-cancer research .

HY-112462

Cdk1/2 Inhibitor III	CDK	Cancer
Cdk1/2 Inhibitor III is a selective *Cdk1/2* inhibitor, with an IC₅₀ of 2.1 μM for CDK1/cyclin B .

HY-151110

*PROTAC CDK12/13 Degrader-1*	PROTACs CDK	Cancer
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase *CDK12/CDK13* dual degrader with the DC₅₀ values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .

HY-151110A

*PROTAC CDK12/13 Degrader-1 TFA*	PROTACs CDK	Cancer
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase *CDK12/CDK13* dual degrader with the DC₅₀ values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .

HY-144981

HQ461	CDK Molecular Glues	Cancer
HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death .

HY-144691

PP-C8	PROTACs CDK	Cancer
PP-C8 is a potent and selective *PROTAC CDK12-Cyclin K* degrader. PP-C8 induces CDK12-Cyclin K degradation with DC₅₀s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .

HY-163944

LL-K12-18	Molecular Glues CDK	Cancer
LL-K12-18 is a two-site molecular glue that enhances the protein-protein interaction of the *CDK12-DDB1* complex, stabilizing the *CDK12-DDB1* complex and promoting the degradation of cyclin K (EC₅₀=0.37 nM). LL-K12-18 exhibits strong gene transcription inhibition and anti-proliferation effects in tumor cells. LL-K12-18 can be used in cancer research .

HY-144977

dCeMM4	Molecular Glues CDK	Cancer
dCeMM4 (Compound 5) is a molecular glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .

HY-144976

dCeMM3	Molecular Glues CDK	Cancer
dCeMM3 (Compound 3) is a molecular glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .

HY-157297

CDK-IN-13	CDK	Cancer
CDK-IN-13 (compound 32E) is a potent and selective inhibitor of *CDK12/cyclinK* with an IC₅₀ of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .

HY-144971

dCeMM2	Molecular Glues CDK	Cancer
dCeMM2 (Compound 2) is a molecular glue-type degrader that targets cyclin K. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex .

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-164553

ZSQ836	Apoptosis CDK	Cancer
ZSQ836 is an orally active dual covalent inhibitor of *CDK12/CDK13, with an EC₅₀* value of 32 nM against *CDK12. ZSQ836 can induce apoptosis* and exhibit anticancer activity in vivo. ZSQ836 can be used in the study of ovarian cancer .

HY-168556

YJ9069	CDK PROTACs DNA/RNA Synthesis	Cancer
YJ9069 is a selective CDK12/CDK13 PROTAC degrader with an IC₅₀ of 22.22 nM for in VCaP cells. CDK12/13 degradation rapidly triggers gene-length-dependent transcriptional elongation defects, leading to DNA damage and cell-cycle arrest. YJ9069 effectively inhibits proliferation in subsets of prostate cancer cells and significantly suppresses prostate tumor growth. (Pink: CDK12/CDK13 degradation agent (HY-168658); Black: Linker (HY-W015967); Blue: ligand for E3 ligase (HY-103596)) .

HY-W181530

NCT02	Molecular Glues CDK	Cancer
NCT02 is a cyclin K molecular glue. NCT02 induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. NCT02 has the potential for the research of metastatic colorectal cancer (CRC) .

HY-130250

SR-4835 10+ Cited Publications	CDK Apoptosis	Cancer
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of *CDK12/CDK13* (CDK12: IC₅₀=99 nM, K_d=98 nM; CDK13: K_d=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .

HY-168162

ZLC491	PROTACs CDK	Cancer
ZLC491 is an orally active *CDK12/13* PROTAC degrader. ZLC491 can be used in anticancer research .

HY-103618

THZ531 20+ 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-153244

MFH290	CDK	Cancer
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .

HY-150641

CDK-IN-9	CDK Apoptosis DNA/RNA Synthesis Molecular Glues	Cancer
CDK-IN-9 (compound 24) is a potent *CDK* inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC₅₀ values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .

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-168197

Thalidomide-F-piperidine-piperazine-Cbz	PROTACs	Cancer
Thalidomide-F-piperidine-piperazine-Cbz Conjugate 110 is a conjugate of E3 ligase and linker for the synthesis of CDK12/13 PROTAC degrader (HY-168162) .

HY-139039

BSJ-4-116	PROTACs CDK	Cancer
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and *CDK. BSJ-4-116 is a highly potent and selective CDK12* degrader (PROTAC) with an IC₅₀ of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .

HY-168555

YJ1206	CDK PROTACs Apoptosis	Cancer
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC₅₀ of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .

HY-80013A

THZ1 Hydrochloride Maximum Cited Publications 82 Publications Verification	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-80013

THZ1 Maximum Cited Publications 82 Publications Verification	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-173147

CDK2-IN-42	CDK	Cancer
CDK2-IN-42 (Compound H63) is a *CDK12* inhibitor with an IC₅₀ value of 10 nM. CDK2-IN-42 has anti-ESCC (Esophageal Squamous Cell Carcinoma) cell activity. It can block transcriptional elongation, downregulate the core genes in the G1 phase to induce cell cycle arrest, and alter the CDK12-ATM/ATR-CHEK1/CHEK2 signaling axis, resulting in DNA damage. CDK2-IN-42 can effectively inhibit tumor growth in a xenograft mouse model of human ESCC KYSE150. CDK2-IN-42 holds great promise for research in the field of cancer .

HY-162706

BSJ-5-63	PROTACs CDK	Cancer
BSJ-5-63 is a potent *CDK12, CDK7, CDK9* PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)) .

HY-118310

Xylocydine	CDK	Cancer
Xylocydine is an inhibitor of *CDK1/2, inhibiting CDK* function in various apoptotic processes. Xylocydine specifically blocks CDK1 and CDK2 activity with IC50 of 1.4 nM and 61 nM, respectively. In addition, Xylocydine downregulates phosphorylated nucleolin and retinoblastoma protein levels. .

HY-155038

Antitumor agent-104	PARP CDK	Cancer
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of *CDK12* .

HY-10542

GW 5074 5+ Cited Publications	Raf Apoptosis	Cancer
GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms .

HY-149398

PARP-1/2-IN-2	Apoptosis PARP CDK	Cancer
PARP-1/2-IN-2-IN-1 (Compound 12e) is a *PARP1/2/CDK12* inhibitor (IC₅₀: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .

HY-116871

YKL-1-116	CDK	Cancer
YKL-1-116 is a selective and covalent inhibitor of *Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 ^WT and Cdk7 ^as, although Cdk*7 ^as is relatively resistant to this compound as well .

HY-138293

SY-5609 1 Publications Verification CDK7-IN-3	CDK Apoptosis	Cancer
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent *CDK7* inhibitor with a K_D of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (K_i=2600 nM), CDK9 (K_i=960 nM), CDK12 (K_i=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity .

HY-149819

CDK/HDAC-IN-3	HDAC CDK	Cancer
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .

HY-151878

CDK7-IN-20	CDK GSK-3	Metabolic Disease
CDK7-IN-20 is a potent, selective and irreversible *CDK7* (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research .

Species:	Human (6)
Tag:	His (2) Tag Free (1) GST (5) Flag (3)
Source:	Sf9 insect cells (6)

Cat. No.	Compare	Product Name	Species	Source

HY-P701361

	CDK12-CCNK Heterodimer Protein, Human (Sf9, GST, FLAG) CDK12; CCNK; Cyclin-dependent kinase 12; Cdc2-related kinase; arginine/serine-rich; CrkRS; Cell division cycle 2-related protein kinase 7; CDC2-related protein kinase 7; Cell division protein kinase 12; hCDK12; Cyclin-K	Human	Sf9 insect cells
	The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (Sf9, GST, FLAG) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by Sf9 insect cells , with N-Flag, N-GST labeled tag.

HY-P701360

	CDK12-CCNK Heterodimer Protein, Human (Sf9) CDK12; CCNK; Cyclin-dependent kinase 12; Cdc2-related kinase; arginine/serine-rich; CrkRS; Cell division cycle 2-related protein kinase 7; CDC2-related protein kinase 7; Cell division protein kinase 12; hCDK12; Cyclin-K	Human	Sf9 insect cells
	The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK12-CCNK Heterodimer protein, expressed by Sf9 insect cells , with tag free.

HY-P702692

	CDK12-CCNT1 Protein, Human (sf9, GST, Flag, His) CDK12; CCNK; Cyclin-dependent kinase 12; Cdc2-related kinase; arginine/serine-rich; CrkRS; Cell division cycle 2-related protein kinase 7; CDC2-related protein kinase 7; Cell division protein kinase 12; hCDK12; Cyclin-K	Human	Sf9 insect cells
	The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNT1 Protein, Human (sf9, GST, Flag, His) is the recombinant human-derived CDK12-CCNT1, expressed by Sf9 insect cells , with N-His, N-GST, N-Flag labeled tag. ,

HY-P702885

	CDK12-CCNK Protein, Human (658-1490,sf9, GST) CRK7; CRKRS; KIAA0904	Human	Sf9 insect cells
	The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Protein, Human (658-1490,sf9, GST) is the recombinant human-derived CDK12-CCNK, expressed by Sf9 insect cells , with N-GST labeled tag. ,

HY-P702886

	CDK12-CCNK Protein, Human (696-1082, sf9, GST) CRK7; CRKRS; KIAA0904	Human	Sf9 insect cells
	The CDK12 protein is a cyclin-dependent kinase that critically phosphorylates the C-terminal domain of POLR2A, thereby regulating transcription elongation. It selectively targets "Ser-5" phosphorylated at "Ser-7" in the CTD repeat and can also target "Ser-2". CDK12-CCNK Protein, Human (696-1082, sf9, GST) is the recombinant human-derived CDK12-CCNK, expressed by Sf9 insect cells , with N-GST labeled tag. ,

HY-P703629

	CDK12-CCNT1 Protein, Human (Active, Sf9, GST, His, Flag) CRK7; CRKRS; KIAA0904	Human	Sf9 insect cells

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